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METHOD FOR THE PREPARATION OF CITALOPRAM
专利权人:
H. LUNDBECK A/S
发明人:
DALL'ASTA, LEONE,CASAZZA, UMBERTO,PETERSEN, HANS
申请号:
HU0104128
公开号:
HU228576B1
申请日:
1999.10.19
申请国别(地区):
HU
年份:
2013
代理人:
摘要:
The present invention relates to a method for the preparation of citalopram or any of its enantiomers and acid addition salts thereof comprising treatment of a compound of formula (IV), wherein X is O or S; R1-R2 are each independently selected from hydrogen and C1-6 alkyl, or R1 and R2 together form a C2-5 alkylene chain thereby forming a spiro-ring; R3 is selected from hydrogen and C1-6 alkyl, R4 is selected from hydrogen, C1-6 alkyl, a carboxy group or a precursor group therefore, or R3 and R4 together form a C2-5 alkylene chain thereby forming a spiro-ring, with a dehydration agent or alternatively where X is S, thermally cleavage of the thiazoline ring, or treatment in presence of a radical initiator, to form citalopram. The invention also relates to intermediates used in the new process for the preparation of citalopram, as well as citalopram prepared according to the new process.
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