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Method for preparing Salt type camsilate
专利权人:
ASTRAZENECA AB
发明人:
CRAIG ROBERT STEWART,MARTIN HANS BOHLIN
申请号:
ARP160101953
公开号:
AR105176A2
申请日:
2016.06.28
申请国别(地区):
AR
年份:
2017
代理人:
摘要:
Un procedimiento de preparaci n de una sal de tipo camsilato de (1r 1R 4R) -4-metoxi-5-metil-6- 5- (prop-1-in-1-il) piridin-3-il -3H-diespiro 1. Hexano-1, 2-indeno-12-imidazol] - 4-amine with acid (1s) -(+) - 10-camforsulfoni 1. Characteristic 1: prepare from (1R, 1R, 4R) - 4-methyl-5-methyl-6 - [5 - (prop-1-in-1-il) piridin-3-il] - 3H diespiro [cyclohexane-1, 2-indo-12-imidazol] - 4-amine de formula (1)characterized in that the process comprises reacting (1r, 1R, 4R) -4-methoxy-5-methyl-6- [5- (prop-1-in-1-yl) pyridin-3-yl] -3H-diespiro [ cyclohexane-1,2-indene-12-imidazole] -4-amine of formula (2) with (1S) - (+) - 10-camforsulfonic of formula (3). Claim 2: The process according to claim 1, characterized in that the compound (1r, 1R, 4R) -4-methoxy-5-methyl-6- [5- (prop-1-in-1-yl) pyridin-3- il] -3H-diespiro [cyclohexane-1,2-indene-12-imidazole] -4-amine is prepared according to a method comprising reacting the salt of (+) - 10-camphorsulfonic acid of (1r, 4r) - 6-bromo-4-methoxy5-methyl-3h-dispiro [cyclohexane-1, 2-indeno-1, 2-pyridan] - 4-diamine (4) and 5-acid (prop-1-inil) pyridine-3-ilboronic (5) have a transition metal catalyst and a substrate. Claims 5: procedures on which any claim is based 1-4characterized in that said (+) - 10-camforsulfonic acid salt of (1r, 4r) -6-bromo-4-methoxy-5-methyl-3H-dispiro [cyclohexane-1,2-indene-1,2-imidazole] -4-amine is prepared according to a procedure comprising reacting (1r, 4r) -6-bromo-4-methoxy-5-methyl-3H-diespiro [cyclohexane-1,2-indene-12-imidazole] -4 ( 3H) -thion of formula (6) with ammonia in the presence of zinc acetate dihydrate, followed by the addition of (1S) - (+) - 10-camphorsulfonic acid. Claim 6: The method according to claim 5,The compound (1R, 4R) - 6-bromo-4-methoxy-5-methyl-3h-diespiro [cyclohexane-1, 2-indo-12-imidazol] - 4 (3H) - Iona was prepared by a process including the reaction of hydrochloric acid (1R, 4R) - 6-bromo-4-methospiro [cyclohexane-1, 2-indo] - 1 (3H) - with 2-oxpanotia (7).Un p
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