Category: 114312-57-1

On April 23, 2020, Luo, Huichao; Ren, Qingyun; Yin, Junjun; Wu, Chunlin; Fan, Yuxin; Mo, Yufeng; Zhang, Yingjun published a patent.HPLC of Formula: 114312-57-1 The title of the patent was Oxazinopyridotriazinediones as influenza virus replication inhibitor and their preparation. And the patent contained the following:

The invention belongs to the field of medicine, and particularly relates to a compound of formula I as a replication inhibitor of influenza virus and a preparation method thereof, a pharmaceutical composition comprising the compound and use of the compound and pharmaceutical composition thereof in treating influenza. The invention provides a compound having formula I or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, that can inhibit influenza virus well, and/or has lower cytotoxicity, better in vivo pharmacokinetic properties and in vivo pharmacodynamic properties. Compounds of formula I wherein Y is O, S, SO, SO2, CR7R8 and NH and derivatives; ring Cy is C3-5 carbocyclic ring, 3- to 8-membered heterocyclic ring and 5- to 10-membered heteroaromatic ring; R1, R2, R3, R4, R5 and R6 are independently H, D, Cl, Br, I, CN, CO2H, etc.; R7 and R8 are independently H, D, F, I, CN, NO2, NH2, etc.; m is 0, 1, 2, 3, and 4; each Rx is independently H, D, F, Br, NO2, C1-6 alkyl, etc.; and stereoisomers, tautomers, N-oxides, solvates, metabolites, pharmaceutically acceptable salts and prodrugs thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compound were evaluated for their influenza virus replication inhibitory activity. From the assay, it was determined that compound II exhibited EC50 value of 4.27 nM. The experimental process involved the reaction of Ethyl 3-fluoro-2-methylbenzoate(cas: 114312-57-1).HPLC of Formula: 114312-57-1

The Article related to oxazinopyridotriazinedione preparation influenza virus replication inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Triazines and other aspects.HPLC of Formula: 114312-57-1

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On June 24, 2021, Morrow, Benjamin Joseph; Hubert, Jonathan Grant; Stupple, Paul Anthony; Camerino, Michelle Ang; Dennis, Matthew Lloyd; Cuzzupe, Anthony Nicholas published a patent.Application In Synthesis of Ethyl 3-fluoro-2-methylbenzoate The title of the patent was preparation of heteroaryl compounds useful for producing drugs in the treatment or prevention of diseases ameliorated by the modulation of STING. And the patent contained the following:

This disclosure relates to compounds (e.g., I) which are modulators of STING. Also disclosed are pharmaceutical compositions comprising compounds and methods of using compounds in the treatment or prevention of diseases ameliorated by the modulation of STING. The experimental process involved the reaction of Ethyl 3-fluoro-2-methylbenzoate(cas: 114312-57-1).Application In Synthesis of Ethyl 3-fluoro-2-methylbenzoate

The Article related to heteroaryl modulation sting preparation, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Application In Synthesis of Ethyl 3-fluoro-2-methylbenzoate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On February 18, 2022, Lin, Zhaiwei; Cui, Baicheng published a patent.Formula: C10H11FO2 The title of the patent was Preparation of pyridazinone derivatives and its application as anti-influenza drugs with CEN inhibitory effect. And the patent contained the following:

The present invention relates to the preparation of pyridazinone derivatives and its application as anti-influenza drugs with CEN inhibitory effect. In particular, the pyridazinone derivative I (wherein, R1 = H or -C(=O)Y1, -C(=O)-O-Y1, -(CH2)-O-(C=O)-Y1 etc.; Y1 = optionally substituted C1-10 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted aryl, -C(R* )2NHR** etc., and each R* and R** = independently hydrogen or optionally substituted C1-6 alkyl; R2 and R3 = independently H, D, C1-6 alkyl, -C(O)- C1-6 alkyl, halogen, -OR* etc.; R2 and R3 can be connected to form a ring to form an optionally substituted cycloalkyl, an optionally substituted heterocyclyl and an optionally substituted cycloalkenyl; R* and R** = independently H and optionally substituted C1-6 alkyl; q = 0-6). Further, (R4 = R6 and R7 substituted isobutane, where R6 and R7 are optionally substituted aryl groups and optionally substituted heteroaryl groups; wherein the substituents are independently C1-6 alkyl, -CN, -COOR* etc., where R* and R** = independently H, D and optionally substituted C1-6 alkyl; q = 0-6; R6 and R7 can be linked to form a compound II (wherein, m and n = independently 0-3, Q = CR*R**, NR*, O, S, SO, SO2; R* and R** = independently H, D and optionally substituted C1-6 alkyl); R5 = optionally substituted cycloalkyl, optionally substituted heterocyclyl and optionally substituted cycloalkenyl, such as a 6-membered ring, the ring may be carbocycle or O, N containing heterocycle) or its pharmaceutically acceptable salts, solvates, including hydrates, polymorphs, prodrugs, co-crystals, tautomers, stereoisomers were prepared The inventive compounds can be used as anti-influenza drugs having CEN inhibitory action. The experimental process involved the reaction of Ethyl 3-fluoro-2-methylbenzoate(cas: 114312-57-1).Formula: C10H11FO2

The Article related to pyridazinone derivative preparation antiinfluenza drug cen inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Formula: C10H11FO2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On April 5, 2022, Wang, Yonggang; Lin, Zhaiwei; Hu, Shuanghua published a patent.Safety of Ethyl 3-fluoro-2-methylbenzoate The title of the patent was Preparation of pyridazinone derivatives and its application thereof. And the patent contained the following:

The present invention relates to the preparation of pyridazinone derivatives and its application thereof. In particular, pyridazinone derivative I (wherein, R1 is H, optionally substituted phosphate group or -C(=O)Y1, -C(=O)-O-Y1, -(CH2)-O-(C=O)-Y1, (CH2)- O-(C=O)-O-Y1, -(CHCH3)-O-(C=O)-Y1 and -(CHCH3)-O-(C=O)-O-Y1; Y1 is optionally substituted C1-10 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted aryl, etc.; R2 and R3 can be optionally independently H, C1-6 alkyl, -C(O)-C1-6 alkyl, halogen, -CF3, -CN, etc.; R4 is (R7)(R8)CH- (here, R7 and R8 are are optionally substituted aryl, and optionally substituted heteroaryl; wherein the substituents are independent C1-6 alkyl, -C(O)- C1-6 alkyl, etc.)). Further, (or II (here, R9, R10 are optionally substituted aryl, and optionally substituted heteroaryl; wherein the substituents are independent C1-6 alkyl, -C(O)- C1-6 alkyl, C1-6 haloalkyl, halogen, -CF3, etc.; R11 is H, C1-3 alkyl, C1-3 haloalkyl or C1-3 alkoxy); R7 and R8 can be linked to form a ring structure III (where n and m can be independently 0-3, Q is CR*R**, NR*, O, S, SO, SO2; R* and R** are independently H and optionally substituted C1-6 alkyl); R5 and R6 are independently selected from F, CH3 and CF3, and R5 and R6 are not selected as CH3 at the same time) and its pharmaceutically acceptable salts, solvates, hydrates, N-oxides, polycrystals, prodrugs, co-crystals, tautomers, stereoisomers or their mixtures, isotopically labeled derivatives were prepared The inventive compounds of the present invention can be used as anti-influenza drugs having CEN (cap-dependent endonuclease) inhibition. The experimental process involved the reaction of Ethyl 3-fluoro-2-methylbenzoate(cas: 114312-57-1).Safety of Ethyl 3-fluoro-2-methylbenzoate

The Article related to pyridopyridazine dione derivative preparation antiinfluenza drug, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Safety of Ethyl 3-fluoro-2-methylbenzoate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On February 18, 2022, Lin, Zhaiwei; Cui, Baicheng published a patent.Name: Ethyl 3-fluoro-2-methylbenzoate The title of the patent was Preparation of pyridazinone derivative and its application for preventing, alleviating or treating viral infection. And the patent contained the following:

The present invention relates to the preparation of pyridazinone derivative and its application for preventing, alleviating or treating viral infection. In particular, the pyridazinone derivatives I (wherein, R1 = H or -C(=O)Y1, -C(=O)-O-Y1, -(CH2)-O-(C=O)-Y1, -(CH2)-O-(C=O)-OY1, -(CHCH3)-O-(C=O)-Y1 and -(CHCH3)-O-(C=O)-O-Y1; Y1 is optionally substituted C1-10 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, monosubstituted amino, disubstituted amino, and -C(R*)2NHR**; and each R* and R** is independently hydrogen or optionally substituted C1-6 alkyl; R2 and R3 = H, D, C1-6 alkyl, -C(O)-C1-6 alkyl, halogen, -CF3, -CN, -COOR*, -OR*, (CH2)qNR*R**, -C(O)-NR*R**; R4 is (un)substituted (hetero)arylmethyl). On further, ( R2 and R3 can be connected to form a ring to form an optionally substituted cycloalkyl, an optionally substituted heterocyclyl and an optionally substituted cycloalkenyl; R* and R** are independently H and optionally substituted C1-6 alkyl; q is 0-6; R7 and R8 are optionally substituted aryl, and optionally substituted heteroaryl; wherein the substituents are independent C1-6 alkyl, -C(O)-C1-6 alkyl, halogen, -CF3, – CN, -COOR*, -OR*, -(CH2)qNR*R**,-C(O)-NR*R**; R* and R** = H, D and optionally substituted C1-6 alkyl, q is 0-6; R7 and R8 can be linked to form the structure III; n and m = 0-3, Q = CR*R**, NR*, O, S, SO, SO2; and R* and R** are independently H and optionally substituted C1-6 alkyl) and its pharmaceutically acceptable salts, solvates, hydrates, polycrystals, prodrugs, co-crystals, tautomers, and stereoisomers thereof was prepared More specifically, the compounds of the present invention can be used as anti-influenza drugs with CEN inhibitory effect. The experimental process involved the reaction of Ethyl 3-fluoro-2-methylbenzoate(cas: 114312-57-1).Name: Ethyl 3-fluoro-2-methylbenzoate

The Article related to pyridazinone derivative preparation viral infection treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Name: Ethyl 3-fluoro-2-methylbenzoate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On January 4, 2022, Hu, Shuanghua; Lin, Zhaiwei; Cui, Baicheng published a patent.Name: Ethyl 3-fluoro-2-methylbenzoate The title of the patent was Preparation of pyridazinone derivatives and its application as anti-influenza drugs with CEN inhibitory effect. And the patent contained the following:

The present invention relates to the preparation of pyridazinone derivatives and its application as anti-influenza drugs with CEN inhibitory effect. In particular, the pyridazinone derivative I (wherein, R1 = H or, -C(=O)Y1, -C(=O)-O-Y1, etc.; Y1 = optionally substituted C1-10 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted aryl, etc.; where R* and R** = H or optionally substituted C1-6 alkyl; R2 and R3 = H, C1-6 alkyl, -C(O)-C1-6 alkyl, etc.; where R* and R** = H and optionally substituted C1-6 alkyl; q is 0-6; R4 = compound II; R9 and R10 = optionally substituted aryl, and optionally substituted heteroaryl; wherein the substituents are independent C1-6 alkyl, -C(O)- C1-6 alkyl, etc.; where R* and R** = H and optionally substituted C1-6 alkyl, and q is 0-6; R9 and R10 = linked to form the compound III; wherein n and m = 0-3, Q = CR*R**, NR*, O, S, SO, SO2; R* and R** = H and optionally substituted C1-6 alkyl;). Further, (R5 and R6 = H, or is selected from optionally substituted C1-8 alkyl, optionally substituted C2-8 alkenyl, etc.; wherein R* and R** = H and optionally substituted C1-6 alkyl, and q is 0-6; R7 and R8 = H, C1-6 alkyl, -C(O)- C1-6 alkyl, etc.; R* and R** = H and optionally substituted C1-6 alkyl; q is 0-6; R5, R7 or R6, R8 can be connected into a 5-8 membered saturated or unsaturated ring, such as a 6-membered ring, the ring may be a carbocyclic ring, or a heterocyclic ring containing O or N) or its pharmaceutically acceptable salts, solvates, hydrates, polycrystals, prodrugs, co-crystals, tautomers, stereoisomers, were prepared The inventive pyridazinone derivatives can be used as anti-influenza drugs with CEN inhibitory effect. The experimental process involved the reaction of Ethyl 3-fluoro-2-methylbenzoate(cas: 114312-57-1).Name: Ethyl 3-fluoro-2-methylbenzoate

The Article related to pyridazinone derivative preparation antiinfluenza drug cen inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Name: Ethyl 3-fluoro-2-methylbenzoate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On September 7, 2001, Yamabe, Haruko; Okuyama, Masahiro; Nakao, Akira; Ooizumi, Mitsuru; Saito, Ken-ichi published a patent.Computed Properties of 114312-57-1 The title of the patent was Preparation of cyclic amide derivatives as sigma receptor ligands. And the patent contained the following:

The title compounds I [X is alkyl, aryl, a heterocyclic group, etc.; Q is CH2, CO, O, etc.; n is an integer of 0 to 5; R1 and R2 are each hydrogen, alkyl, etc.; and B is Q1, etc.; A = (CH2)m; R3, R4, R5 and R6 are each hydrogen, halogeno, alkoxy, etc.; m is 1 or 2] are prepared In an in vitro test for inhibition of sigma-2 receptor binding, 4-bromo-2-[[1-[2-(4-fluorophenyl)-2-oxoethyl]piperidin-4-yl]methyl]isoindolin-1-one hydrochloride showed the Ki value of 2.8 nM. Formulations are given. The experimental process involved the reaction of Ethyl 3-fluoro-2-methylbenzoate(cas: 114312-57-1).Computed Properties of 114312-57-1

The Article related to cyclic amide preparation sigma receptor ligand, isoindolinone preparation sigma receptor ligand, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Computed Properties of 114312-57-1

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On January 21, 2010, Lee, Eun Kyung; Schoenfeld, Ryan Craig; Weikert, Robert James published a patent.Name: Ethyl 3-fluoro-2-methylbenzoate The title of the patent was Indole and indazole derivatives as monoamine reuptake inhibitors and their preparation, pharmaceutical compositions and use in the treatment of depression and anxiety. And the patent contained the following:

The invention discloses indole and indazole derivatives of formula I and their pharmaceutically acceptable salts, which are useful for treatment of diseases associated with monoamine deficiency. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds Compounds of formula I wherein A is CH, CR2 and N; Q is CH, CR1 and N; X is CH2, CH(OH) and CO; Y is (CHR5)0-2 and O(CHR5)0-2; Z1 is CH, N and CR3; Z2 is CH, S and CR3; B is (CH)0-1; R1 and R2 are independently CN, CONH2, SO2H, SO2-lower alkyl, halo, lower (halo)alkyl and lower alkoxy; R3 is lower (halo)alkyl, lower alkoxy, halo, CN, CONH2 and derivatives, NHSO2H, NHSO2-lower alkyl, and NH2 and derivatives; R4 is heterocycloalkyl and NH2 and derivatives; R5 is H, lower (hydroxy)alkyl, lower alkoxy and lower haloalkyl; with the proviso that if X is CO, Y is O(CH2)2, A, B, Q, Z1 and Z2 are CH, R1 and R3 are absent, R4 is NH(C(CH3)3), then R2 is a substitute; and their pharmaceutically acceptable salts and esters thereof, are claimed. Example compound II was prepared by a multi-step procedure starting from 2-(tert-butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-8-carboxylic acid (procedure given). All the invention compounds were evaluated for their monoamine reuptake inhibitory activity. From the assay, it was determined that II exhibited the pKi values of 5.93, 6.41 and 6.95 against SERT, NEt and DAT, resp. The experimental process involved the reaction of Ethyl 3-fluoro-2-methylbenzoate(cas: 114312-57-1).Name: Ethyl 3-fluoro-2-methylbenzoate

The Article related to indole indazole preparation monoamine reuptake inhibitor treatment depression anxiety, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Name: Ethyl 3-fluoro-2-methylbenzoate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On September 18, 2008, Mochizuki, Akiyoshi; Kishida, Masamichi; Kanno, Hideyuki published a patent.Recommanded Product: Ethyl 3-fluoro-2-methylbenzoate The title of the patent was Preparation of diamide derivatives as FXa inhibiting antithrombotics. And the patent contained the following:

The title compounds I [ring A = benzene ring, pyridine ring, pyrimidine ring, etc.; R1 = H, halo, alkyl, etc.; R2 = H, carboxy, carbamoyl, etc.; T1 = N(R3)CO; R3 = H, alkyl; T2 = (CH2)mCONH; m = 1 or 2; Q1 = cyclohexyl, morpholinyl, pyrrolidinyl, etc.; Q2 = single bond, 1,4-phenylene, 1,4-cyclohexylene, etc.; Q3 = (un)substituted Ph, thienyl, pyridyl, etc.] are prepared Thus, 4-[4-(2-([(5-chlorothiophene-2-carbonyl)amino]methyl]phenylcarbamoyl)phenyl)-3-oxopiperazine-1-carboxylic acid tert-Bu ester was prepared from N-(2-aminobenzyl)-5-chlorothiophene-2-carboxamide and 4-(2-[N-tert-butoxycarbonyl-N-(carboxymethyl)amino]ethylamino)benzoic acid. Compounds of this invention showed IC50 values of 1.1 nM to 8.8 nM against human FXa. The experimental process involved the reaction of Ethyl 3-fluoro-2-methylbenzoate(cas: 114312-57-1).Recommanded Product: Ethyl 3-fluoro-2-methylbenzoate

The Article related to amide derivative preparation fxa inhibitor antithrombotic, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: Ethyl 3-fluoro-2-methylbenzoate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On December 30, 1987, Uno, Hitoshi; Kurokawa, Mikio; Sato, Fiminori; Naruto, Shunsuke; Masuda, Yoshinobu published a patent.Synthetic Route of 114312-57-1 The title of the patent was Processes for the preparation of 11-piperazinyl-6,11-dihydrodibenz[b,e]oxepins as antianoxia agents. And the patent contained the following:

Title compounds I [R1 = H, MeO; R2 = H, MeO, HO, F; R3 = H, F; R4 = H, 7-, 8-, 9-F; Ar = Ph, thienyl, pyridyl] and their physiol. acceptable salts are prepared from II [R1, R3, R4 = same as I; R2 = H, MeO, (protected) HO, F, reactive ester residue (O is attached to the rings)] and III (Ar = same as I). (E)-III (Ar = Ph) (4.0 g) was treated with 2.0 g II (R1 = R2 = R4 = H, R3 = F, Y = Cl) (preparation given) in CHCl3 at room temperature for 2 h to give 1.5 g (E)-I (R1 = R2 = R4 = H, R3 = F, Ar = Ph), which was converted into the maleate salt monohydrate (IV). IV showed cerebral antianoxia activity at min. ED of 10 mg/kg p.o. in ischemic mice and life-prolongation activity for anoxia at 100 mg/kg in mice, vs. > 100 mg/kg p.o. and no life-prolongation activity, resp., for I (R1 = R2 = R4 = H, R3 = Me, Ar = Ph) dioxalate hydrate (V). A film-coated tablet containing IV 5, corn starch 33, lactose 75, cellulose 30, hydroxypropylcellulose 5, SiO2 1, and Mg stearate 1 g was prepared The experimental process involved the reaction of Ethyl 3-fluoro-2-methylbenzoate(cas: 114312-57-1).Synthetic Route of 114312-57-1

The Article related to piperazinyl dihydro dibenzoxepin preparation antianoxia, dibenzoxepin piperazinyldihydro preparation antianoxia, oxepin piperazinyldihydrodibenzoxepin preparation antianoxia and other aspects.Synthetic Route of 114312-57-1

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics