HORMANN Robert E. (US),ХОРМАНН Роберт И. (US),LI Bing (US),ЛИ Бинг (US)
申请号：
RU2013121780
公开号：
RU0002640807C2
申请日:
2013.05.06
申请国别(地区):
RU
年份:
2018
代理人:
摘要：
FIELD: biotechnology.SUBSTANCE: invention relates to a method for preparation of an enantiomerically enriched compound with Formula III , wherein A is (C1-C6)alkyl-O-, phenyl- C1-C6)alkyl-O-； aryl selected from phenyl, naphthyl, benzo 1,3]dioxole, 2,3-benzo[1,4]dioxin which is optionally substituted by 1 to 3 substituents, where the substituents are selected from (C1-C6) alkyl, (C3-C7) cycloalkyl, (C1-C6)alkyl-O-, hydroxy, amino and halo； or heteroaryl having four or five carbon atoms and one heteroatom selected from oxygen, nitrogen and sulfur, which is optionally substituted by 1 to 3 substituents, where the substituents are selected from (C1-C6)alkyl, (C3-C7)cycloalkyl, (C1-C6)alkyl-O-, hydroxy, amino and halo； B is phenyl optionally substituted by 1 to 3 substituents, where the substituents are selected from (C1-C6)alkyl, (C3-C7)cycloalkyl, (C1-C6)alkyl-O-, hydroxy, amino and halo； and R1 and R2 independently represent (C1-C6)alkyl, phenyl-(C1-C6)alkyl-, hydroxy-(C1-C6)alkyl, (C3-C7)cycloalkyl, (C2-C6)alkenyl or (C2-C6)alkynyl； provided that R1 differs from R2； where the absolute configuration of the asymmetric carbon atom carrying R1 and R2, is an R-configuration； including (a) reaction of Formula XI acylhydrazine with Formula XII ketone to form a compound of Formula XIII , where R1 differs from R2, (b) reduction of the Formula XIII compound in the presence of a chiral catalyst to form a Formula R-XIV compound and (c) reaction of the Formula R-XIV compound with the Formula B-CO-LG compound, wherein LG is a leaving group, forming a compound with Formula III.EFFECT: chiral diacylhydrazine ligands for genome modulation.6 cl, 25 dwg, 11 tblИзобретение относится к способу получения энантиомерно обогащенного соединения, имеющего Формулу III, где А представляет собой (С1-С6)алкил-O-, фенил-(С1-С6)алкил-O-； арил, выбранный из фенила, нафтила, бензо[1,3]диоксола, 2,3-бензо[1,4]диоксина, который возможно замещен 1-3 заместителями, где заместители выбраны из (С1-С6)алк
