On July 17, 2014, Campos, Sebastien Andre; Harling, John David; Miah, Afjal Hussain; Smith, Ian Edward David published a patent.Recommanded Product: 882518-89-0 The title of the patent was Proteolysis targeting chimeras (protacs) directed to the modulation of the estrogen receptor. And the patent contained the following:
The invention relates to compounds I [wherein L is a linking group comprising a length of 6-16 atoms in shortest length having the formula (CH2)n(R1CH2CH2)m(OCH2)qCONH; n = 0-6; m = 2-10; q = 0 or 1; each R1 is independently O, NH, N(C1-3-alkyl), or a 4-6 membered heterocyclyl group containing 2 N atoms linked to the carbons in the chain via the ring N atoms (optionally substituted by oxo).; R2 is straight or branched C1-6-alkyl or C3-6-cycloalkyl; X is oxazol-5-yl or 2-R4-4-R3-thiazol-5-yl; R3 is H or CH3; R4 is H or CH3; and R5 is OH or O-(C1-3-alkyl)], or a pharmaceutically acceptable salt thereof. The invention also relates to processes for the preparation of said compounds, compositions, combinations and medicaments containing said compounds and the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor. Thus, protac II was prepared from 16-((7R,8R,9S,13S,14S,17S)-3,17-dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-7-yl)-3,6,9,12-tetraoxahexadecan-1-oic acid (III) via amidation with (2S,4R)-1-((S)-2-amino-3-methylbutanoyl)- 4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride (IV.HCl); the preparations of III and IV are also presented. All compounds showed evidence of ERα degradation in this assay relative to the DMSO control at 1 uM. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Recommanded Product: 882518-89-0
The Article related to estrane steroids amino acid conjugate preparation modulation estrogen receptor, proteolysis targeting chimera estratriene preparation modulation estrogen receptor, Steroids: Estranes and other aspects.Recommanded Product: 882518-89-0
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics