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Acid (+) - 1,4-dihydro-7 - [(3S, 4S) - 3-methoxy-4 - (methylamine) - 1-pyridine-1 - (2-sulfur) 1,8-nafiridin-3-methoxyethane
专利权人:
SUNESIS PHARMACEUTICALS; INC.
发明人:
申请号:
ARP170101388
公开号:
AR108558A2
申请日:
2017.05.23
申请国别(地区):
AR
年份:
2018
代理人:
摘要:
1. For the production of (+ - 1,4-dihydro-7 - [(3S, 4S) - 3-methoxy-4 - (methylamine) - 1-pyridine-1 - (2-thiazolpidan) - 1,8-naftiridin-3-carboxyl; It also includes acid (+ - 1,4-dihydro-7 - [(3S, 4S) - 3-methoxy-4 - (methylamine) - 1-pyridine-4] - 4-2. Oxo-1 - (2-tiazolyl) - 1,8-naftiridin-3-carboxyl and the treatment method using these compounds. 1. Characteristic 1: a product for the production of (+ - 1,4-dihydro-7 - [(3S, 4S) - 3-methoxy-4 - (methylamine) - 1-pyridyl-4 -- 4 - (methylamine) - 1-hydroxy-1 - (2-thiazolidine) - 1,8-nafiridin-3-carboxyIts characteristics are as follows: a formula compound (1) and ethylene oxide of methylamine are opened to obtain a formula compound (2),ii) resolving the compound of formula (2) with a chiral acid selected from L - (-) - malic acid and L - (-) - pyroglutamic acid to obtain the compound of formula (3) or (4),iii) protecting the secondary amine of the compound of formula (3) or (4) with the tert-butoxycarbonyl protecting group to obtain the compound of formula (5),iv) methylating the free hydroxyl group of the compound of formula (5) with a methylating agent, v) deprotecting the amino groups with p-toluenesulfonic acid monohydrate to obtain the compound of formula (6),vi) reacting the compound of formula (6) with the compound of formula (7) to obtain (+) - 1,4-dihydro-7 - [(3S, 4S) -3-methoxy-4- (methylamino) -1-pyrrolidinyl] -4-oxo-1- (2-thiazolyl) -1,8-naphthyridin-3-carboxylic. Claim 42: A compound characterized in that it is selected from the compounds of formula (3) or (4).Métodos para preparar ácido (+)-1,4-dihidro-7-[(3S,4S)-3-metoxi-4-(metilamino)-1-pirrolidinil]-4-oxo-1-(2-tiazolil)-1,8-naftiridin-3-carboxílico. También composiciones farmacéuticas que comprenden ácido (+)-1,4-dihidro-7-[(3S,4S)-3-metoxi-4-(metilamino)-1-pirrolidinil]-4-oxo-1-(2-tiazolil)-1,8-naftiridin-3-carboxílico y métodos de tratamiento que utilizan dichas composiciones. Reivindicación 1: Un proceso para preparar ácido (+)-1,4-dihidro-7-[(
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