SEL D'ADDITION D'ACIDE D'ELAGOLIX ET COMPOSÉS APPARENTÉS

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专利权人:

SANDOZ AG

发明人:

申请号：

EP18201039.7

公开号：

EP3572406A1

申请日:

2018.10.17

申请国别(地区):

EP

年份:

2019

代理人:

摘要：

The current invention discloses preparation of acid addition salts of 4-[2-[5-(2-Fluoro-3-methoxyphenyl)-3-[2-fluoro-6-(trifluoromethyl)benzyl]-4-methyl-2,6-dioxo-1,2,3,6-tetrahydro-1-pyrimidinyl]-1(R)-phenylethylamino]butyric acid by treatment of an acid-sensitive ester of , 4-[2-[5-(2-Fluoro-3-methoxyphenyl)-3-[2-fluoro-6-(trifluoromethyl)benzyl]-4-methyl-2,6-dioxo-1,2,3,6-tetrahydro-1-pyrimidinyl]-1 (R)-phenylethylamino]butyric acid with a sufficiently strong acid and subsequent isolation by filtration. The process of the invention prevents formation of (R)-5-(2-fluoro-3-methoxyphenyl)-1-(2-fluoro-6-(trifluoromethyl)benzyl)-6-methyl-3-(2-(2-oxopyrrolidin-1-yl)-2-phenylethyl)pyrimidine-2,4(1H,3H)-dione (Va).

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