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METHOD OF PRODUCING SGLT2 INHIBITORS
专利权人:
INK.;TERAKOS
发明人:
LIU Dzhejson (US),ЛИУ Джейсон (US),U Juehlin (CN),У Юэлин (CN),LI Shenbin' (CN),ЛИ Шенбинь (CN),SJuJ Geh (CN),СЮЙ Гэ (CN),LIU DZHEJSON,ЛИУ Джейсон,U JUEHLIN,У Юэлин,LI SHENBIN,ЛИ Шенбинь,SJUJ GEH,СЮЙ Гэ
申请号:
RU2011110691/04
公开号:
RU0002530494C2
申请日:
2009.08.21
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: present invention relates to a method of producing a complex of formula amino acid IA ,wherein the amino acid is selected from a group consisting of proline and phenylalanine, where n is equal to 1 or 2; R1 is selected from a group consisting of hydrogen and a halogen; V is selected from a group consisting of oxygen and a single bond; W is selected from a group consisting of C1-C6 alkylene, C2-C6 alkenylene, C2-C6 alkynylene and C3-C10 cycloalkylene; X is selected from a group consisting of a single bond and oxygen; Y is selected from a group consisting of hydrogen, C1-C6 alkyl, C1-C2 haloalkyl, C1-C6 hydroxyalkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C10 cycloalkyl, (C3-C10 cycloalkyl)C1-C4 alkyl and (C1-C4 alkyloxy)C1-C3 alkyl, where the alkyl or cycloalkyl groups or parts thereof in W and Y are optionally partially or completely fluorinated, or a pharmaceutically acceptable salt thereof, which includes (a) reacting a compound of formulaIIwith a reducing agent in the presence of an activating agent to form a compound of formula III,(b) contacting said compound of formula III with an amino acid to form said complex of formula IA; where steps (a) and (b) are carried out without purifying said compound of formula III and where steps (a) and (b) are carried out consecutively without intermediate steps of introducing and removing group protection, having inhibiting activity on sodium-dependent transporter SGLT.EFFECT: method reduces the number of steps needed to obtain said compounds and the obtained complexes are usually provided in crystalline form.10 cl, 3 dwg, 1 tbl, 7 exДанное изобретение относится к способу получения комплекса формулы IА:в котором аминокислота выбрана из группы состоящей из пролина и фенилаланина, где n представляет собой 1 или 2; R1 выбран из группы, состоящей из водорода и гало; V выбран из группы, состоящей из кислорода и одинарной связи; W выбран из группы, состоящей из C1-C6 алкилена, C2-C6 алкенилена, C2-C6 алкин
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