Category: 872046-08-7

On October 31, 2006, Sbardella, Gianluca; Bartolini, Sara; Castellano, Sabrina; Artico, Marino; Paesano, Nicola; Rotili, Dante; Spadafora, Corrado; Mai, Antonello published an article.SDS of cas: 872046-08-7 The title of the article was 6-alkylthio-4-[1-(2,6-difluorophenyl)alkyl]-1H-[1,3,5]triazin-2-ones (ADATs): novel regulators of cell differentiation and proliferation. And the article contained the following:

Novel triazine analogs of 5-alkyl-2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydropyrimidin-4(3H)-ones (F2-DABOs), previously described by us as nonnucleoside HIV-1 reverse transcriptase inhibitors (NNRTIs), were tested for their antiproliferative and cytodifferentiating activity on the A-375 human melanoma cell line. Most of the tested derivatives were effective in decreasing cell proliferation, facilitating morphol. differentiation, and reprogramming gene expression. All these effects were reversible upon withdrawal of RT inhibitors. Among the compounds tested, 3f (I) showed the highest antiproliferative effect, whereas compound 6c, although not affecting cell proliferation, is endowed with a strong cytodifferentiating effect, which is probably related to a marked upregulation of the e-cad gene. These results support the potential of NNRTIs as valuable antitumor agents. The experimental process involved the reaction of Methyl 2-(2,6-difluorophenyl)acetate(cas: 872046-08-7).SDS of cas: 872046-08-7

The Article related to antitumor triazinone preparation sar, Pharmacology: Structure-Activity and other aspects.SDS of cas: 872046-08-7

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

On November 19, 2021, Gallo, Rafael D. C.; Duarte, Marcelo; da Silva, Amanda F.; Okada, Celso Y. Jr.; Deflon, Victor M.; Jurberg, Igor D. published an article.Product Details of 872046-08-7 The title of the article was A Selective C-C Bond Cleavage Strategy Promoted by Visible Light. And the article contained the following:

A new visible-light-promoted reaction between aryldiazoacetates ArC(=N2)COOR1 (Ar = Ph, 4-chlorophenyl, 3,5-dimethoxypheny, etc.; R1 = Me, Bn, i-Pr, allyl) and 1,3-diketones R2C(O)CH2C(O)R3 (R2 = Me, 4-chlorophenyl, cyclopropyl, etc.; R3 = Me, Ph, 2-methoxyphenyl, etc.) allows good yields and selectivities for C-C bond insertions, leading to the corresponding 1,4-dicarbonyl compounds R2C(O)C(COOR1)(Ar)CH2C(O)R3 . This transformation is straightforward and highly practical. It tolerates air and moisture and does not require the use of any metals. Mechanistic investigations support the involvement of a key cyclopropanol intermediate derived from an intramol. rearrangement. The experimental process involved the reaction of Methyl 2-(2,6-difluorophenyl)acetate(cas: 872046-08-7).Product Details of 872046-08-7

The Article related to dicarbonyl compound preparation, aryldiazoacetate diketone insertion reaction, General Organic Chemistry: Synthetic Methods and other aspects.Product Details of 872046-08-7

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

Chavan, Subhash P.; Khatod, Harshali S.; Das, Tamal; Vanka, Kumar published an article in 2016, the title of the article was Exploration of the diastereoselectivity in an unusual Grignard reaction and its application towards the synthesis of styryl lactones 7-epi-(+)-goniodiol and 8-epi-(-)-goniodiol.Product Details of 872046-08-7 And the article contains the following content:

An unusual diastereoselective Grignard reaction is explored, where the Grignard reagents are derived from 1,n-dihaloalkanes. A steric bias due to the presence of a quaternary center adjacent to the acetonide ester at the benzylic position is responsible for the formation of an intramolecularly reduced product in almost quant. yield. This steric hindrance is responsible for the diastereoselectivity observed with a variety of aromatic as well as aliphatic esters. The unusual Grignard reaction furnishes long chain secondary alcs. possessing a terminal olefin, which are synthetically important intermediates. As an application of this method, the diastereoselective synthesis of styryl lactones viz. 7-epi-(+)-goniodiol (29) and 8-epi-(-)-goniodiol (30) has been achieved. The experimental process involved the reaction of Methyl 2-(2,6-difluorophenyl)acetate(cas: 872046-08-7).Product Details of 872046-08-7

The Article related to stereoselective grignard synthesis styryl lactone goniodiol, Carbohydrates: Alditols, Cyclitols, Glycerides and other aspects.Product Details of 872046-08-7

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

On December 29, 2011, Deng, Yongqi; Zhu, Liang; Shipps, Gerald W., Jr.; Lo, Sie-Mun; Sun, Binyuan; Huang, Xiaohua; Beinstock, Corey; Cooper, Alan B.; Gao, Xiaolei; Yao, Xin; Zhu, Hugh Y.; Kelly, Joseph M.; Boga, Sobhana Babu; Alhassan, Abdul-Basit; Tagat, Jayaram R.; Mansoor, Umar Faruk; Wilson, Kevin; O’Boyle, Brendan M.; Daniels, Matthew; Schell, Adam; Siliphaivanh, Phieng; Fischer, Christian published a patent.Application of 872046-08-7 The title of the patent was Indazolecarboxamide derivatives as ERK inhibitors and their preparation and use for the treatment of cancer. And the patent contained the following:

The invention relates to indazolecarboxamide derivatives of formula I, which are ERK inhibitors and which are useful in the treatment of cancer. Compounds of formula I wherein R is H, alkyl and hydroxyalkyl; R1 is (un)substituted heterocyclyl, (un)substituted heterocycloalkenyl, (un)substituted aryl and (un)substituted heteroaryl; R2 is H and alkyl; R3′ is (un)substituted piperidinyl, (un)substituted azepanyl, (un)substituted oxazepanyl, etc.; and pharmaceutically acceptable salts, solvates and esters thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). All the invention compounds were evaluated for their ERK inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values of 14.4 nM and 28.1 nM towards cERK and aERK, resp. The experimental process involved the reaction of Methyl 2-(2,6-difluorophenyl)acetate(cas: 872046-08-7).Application of 872046-08-7

The Article related to indazolecarboxamide preparation erk inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Application of 872046-08-7

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

On August 11, 2017, Deng, Zeping; Chen, Fangjun published a patent.Formula: C9H8F2O2 The title of the patent was Preparation method of 2-(2,6-difluorobenzyl)pyrrolidine. And the patent contained the following:

The method relates to using 2-(2,6-difluorophenyl)acetic acid as initial material, carrying out esterification under action of catalyst, coupling in presence of alkali, opening loop with reducing agents, closing loop in presence of alkali, and reducing with reducing agent to obtain target product. The catalyst is one or more of 4-dimethylamino pyridine, p-Me Ph sulfonic acid, sulfuric acid, and/or thionyl chloride; the reducing agent is one or more of sodium borohydride, potassium borohydride, lithium borohydride, sodium cyano borohydride, lithium aluminum hydride, and/or borane. The compound is important medicine intermediate. The experimental process involved the reaction of Methyl 2-(2,6-difluorophenyl)acetate(cas: 872046-08-7).Formula: C9H8F2O2

The Article related to difluorobenzylpyrrolidine preparation, Heterocyclic Compounds (One Hetero Atom): Pyrroles and Pyrrolizines and other aspects.Formula: C9H8F2O2

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

On November 28, 2013, Hamaguchi, Wataru; Kinoyama, Isao; Koganemaru, Yohei; Miyazaki, Takehiro; Kaneko, Osamu; Sekioka, Ryuichi; Washio, Takuya published a patent.COA of Formula: C9H8F2O2 The title of the patent was Preparation of tetrahydroisoquinoline derivatives as modulators of serotonin 5-HT5A receptor for treating dementia and schizophrenia. And the patent contained the following:

To provide an excellent agent for preventing or treating dementia and schizophrenia based on serotonin 5-HT5A receptor regulating action, it was found that a tetrahydroisoquinoline derivative characterized by a structure in which an acylguanidino group binds to a N atom of a tetrahydroisoquinoline ring or the like, and a cyclic group binds to an unsaturated ring has a potent 5-HT5A receptor regulating action and an excellent pharmacol. action based on the regulating action and also discovered that the tetrahydroisoquinoline derivative is useful as an agent for treating or preventing dementia, schizophrenia, and the like, whereby the present invention has been completed. Compounds of formula I [R1 = H, (un)substituted O-alkyl, O-(halogeno-alkyl), or aryl, heteroaryl, cycloalkyl, or cycloalkenyl; R2 = H, alkyl, halogeno-alkyl, halogen, CN, OH, O-alkyl, O-(halogeno-alkyl), alkylene-OH, alkylene-O-alkyl, or cycloalkyl; L = C(R3)(R4)-(CH2)n; R3 and R4 independently = H, alkyl, halogen, OH, or O-alkyl; m = 1-2; n = 0-2], and their pharmaceutically acceptable salts, are prepared Thus, e.g., II was prepared by reaction of 8-(5-chloro-3-fluoropyridin-2-yl)-5-fluoro-1,2,3,4-tetrahydroisoquinoline hydrochloride with DMF. Compounds of the invention were tested for their human 5-HT5A receptor binding inhibition activity, e.g., II showed Ki value of 4.3 nM. The experimental process involved the reaction of Methyl 2-(2,6-difluorophenyl)acetate(cas: 872046-08-7).COA of Formula: C9H8F2O2

The Article related to tetrahydroisoquinoline preparation serotonin 5ht5a receptor dementia schizophrenia, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.COA of Formula: C9H8F2O2

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

On February 24, 2022, Su, Wei-Guo; Zhang, Weihan; Deng, Wei; Yang, Haibin published a patent.Formula: C9H8F2O2 The title of the patent was Preparation of pyrimidinone compounds as RIPK1 kinase inhibitors and uses thereof. And the patent contained the following:

The invention relates to pyrimidinone compounds of formula I and their preparation and use RIPK1 kinase inhibitors. Compounds of formula I wherein R1 is H, C1-6 alkyl, C1-6 haloalkyl, etc.; R2 is H, halo, CN, etc.; Z is O, NR3 and CR4R5; R3 is H and C1-6 alkyl; R4 and R5 are each independently H, halo, CN, etc.; ring A is (un)substituted Ph and 5- to 6-membered heteroaryl; ring B is (un)substituted 5- to 12-membered heteroaryl, p is 0 and 1; and their pharmaceutically acceptable salts, solvates, racemic mixtures, enantiomers, diastereomers and tautomers, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their RIPK1 kinase inhibitor activity (data given). The experimental process involved the reaction of Methyl 2-(2,6-difluorophenyl)acetate(cas: 872046-08-7).Formula: C9H8F2O2

The Article related to pyrimidinone preparation ripk1 kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C9H8F2O2

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

On May 15, 2020, Li, Yitao; Lin, Jian; Xu, Junxing; Xiao, Yu; Liu, Xinshuo published a patent.Related Products of 872046-08-7 The title of the patent was Pyrimidinium compound and preparation method and application thereof. And the patent contained the following:

The pyrimidinium compound is represented for example by formula I or a stereoisomer, a nitrogen oxide and a salt thereof of a pyrimidinium compound represented by the formula, a preparation method of the pyrimidinium compound, and an application thereof as an insecticide in agriculture, and a form of an insecticide composition thereof, and a method for controlling pests using the compounds The experimental process involved the reaction of Methyl 2-(2,6-difluorophenyl)acetate(cas: 872046-08-7).Related Products of 872046-08-7

The Article related to pyrimidinium compound preparation insecticide, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 872046-08-7

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

On August 31, 2013, Camarasa, Marta; Barnils, Christian; Puig de la Bellacasa, Raimon; Teixido, Jordi; Borrell, Jose I. published an article.Category: esters-buliding-blocks The title of the article was A new and practical method for the synthesis of 6-aryl-5,6-dihydropyrido[2,3-d]pyrimidine-4,7(3H,8H)-diones. And the article contained the following:

A one step general synthetic method for the synthesis of 6-aryl-5,6-dihydropyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione derivatives was described. This methodol. is based on treating a 2-aryl-substituted acrylate with a 6-amino-4(3H)-pyrimidinone derivative in the presence of a base under microwave irradiation conditions. The resulting pyrido[2,3-d]pyrimidine derivatives present an aryl substituent at position C6, precisely the one directly related to the biol. activity of such heterocyclic compounds These protocols were extended to other 2-alkyl-substituted and 3-alkyl (or aryl)-substituted acrylate derivatives but with lower yields. The synthesis of the target compounds was achieved by a reaction of 2,6-diamino-4(3H)-pyrimidinone with α-(methylene)benzeneacetic acid Me ester derivatives (acrylate esters), α-methylene-1-naphthaleneacetic acid Me ester, 2-methyl-2-propenoic acid Me ester. 6-Amino-2-(methylthio)-4(3H)-pyrimidinone was also a suitable starting material. The title compounds thus formed included 2-amino-5,8-dihydro-6-(phenyl)pyrido[2,3-d]pyrimidine-4,7(3H,6H)-dione (I) and related substances. The experimental process involved the reaction of Methyl 2-(2,6-difluorophenyl)acetate(cas: 872046-08-7).Category: esters-buliding-blocks

The Article related to pyridopyrimidine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: esters-buliding-blocks

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

On December 29, 2005, Bjoere, Annika; Bonn, Peter; Gran, Ulrik; Kajanus, Johan; Olsson, Christina; Ponten, Fritiof published a patent.Application In Synthesis of Methyl 2-(2,6-difluorophenyl)acetate The title of the patent was Preparation of novel oxabispidine compounds and their use in the treatment of cardiac arrhythmias. And the patent contained the following:

There is provided oxabispidines (shown as I; variables defined below; e.g. N-[2-[7-[(2S)-3-(4-cyanophenoxy)-2-hydroxypropyl]-9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl]ethyl]-1-phenylmethanesulfonamide (shown as II)), which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias. For I: R1 = C1-12 alkyl, -C(O)XR7, -C(O)N(R8a)R5d or -S(O)2R9a; R2 = H, halo, C1-6alkyl, OR13, EN(R14)R15 or, together with R3, carbonyl O; R3 = H, C1-6alkyl or, together with R3, carbonyl O; A = direct bond, -J-, -JN(R19a)-, -JS(O)2N(R19b)-, -JN(R19c)S(O)2-, -JO- (in which latter 4 groups, -J is attached to the oxabispidine ring N); B = -Z{[C(O)]aC(H)(R20a)}b-, -Z[C(O)]cN(R20b)-, -ZN(R20c)S(O)2-, -ZS(O)2N(R20d)-, -ZS(O)n-, -ZO- (in which six groups Z is attached to the C atom bearing R2 and R3), -N(R20e)Z-, -N(R20f)S(O)2Z-, -S(O)2N(R20g)Z- or N(R20h)CO2Z- (in which latter 4 groups, Z is attached to the Ph or pyridyl group); J = C1-6alkylene optionally substituted; Z = a direct bond or C1-4 alkylene; G = CH or N; R4 = � optional -OH, cyano, halo, nitro, C1-6 alkyl (optionally terminated by -N(H)C(O)OR21a), C1-6 alkoxy, -N(R22a)R22b, -C(O)R22c, -C(O)OR22d -C(O)N(R22e)R22f -N(R22g)C(O)R22h, -N(R22i)C(O)N(R22j)R22k, -N(R22m)S(O)2R21b, -S(O)2N(R22n)R22o, -S(O)2R21c, -OS(O)2R21d and aryl; and R41 to R46 = H or C1-3 alkyl; addnl. details including provisos are given in the claims. Methods of preparation are claimed and preparations and/or characterization data for �2 examples of I and many intermediates are included. For example, II was prepared (72 %) from phenylmethanesulfonyl chloride and 4-[[(2S)-3-[7-(2-aminoethyl)-9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl]-2-hydroxypropyl]oxy]benzonitrile, the latter of which was prepared (69 %) by deprotection of tert-Bu [2-[7-[(2S)-3-(4-cyanophenoxy)-2-hydroxypropyl]-9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl]ethyl]carbamate. The example I were tested for primary electrophysiol. effects in anesthetized guinea pigs and exhibit D10 >5.5. The example I were tested in a Rb+-efflux assay for detection of HERG channel blockers and exhibit pIC50 >4.5, e.g. 5.72 for II. The experimental process involved the reaction of Methyl 2-(2,6-difluorophenyl)acetate(cas: 872046-08-7).Application In Synthesis of Methyl 2-(2,6-difluorophenyl)acetate

The Article related to oxabispidine preparation cardiac arrhythmia treatment, oxadiazabicyclononane preparation cardiac arrhythmia treatment, Heterocyclic Compounds (More Than One Hetero Atom): Eight- and Higher-Membered Rings and other aspects.Application In Synthesis of Methyl 2-(2,6-difluorophenyl)acetate

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