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PROCESS FOR THE SYNTHESIS OF ARFORMOTEROL
专利权人:
发明人:
HALDAVANEKAR VAMAN VAISHALI,PRABHU MANGESH,RAO DHARMARAJ RAMACHANDRA,KANKAN RAJENDRA NARAYANRAO
申请号:
IN2468/MUMNP/2010
公开号:
IN2010MN02468A
申请日:
2010.11.22
申请国别(地区):
IN
年份:
2014
代理人:
摘要:
The present invention provides a process tor preparing a compound ot" formula (VI) or a salt thereof, the process.comprising: (i) reacting 4-merhoxyphenyl acetone with an amine of formula (VOX) tinder conditions of reductive animation to pro-duce a compound of formula (II) or a salt thereof, wherein there is no isolation of an imine intermediate formed during the reduc-live amination (ii) condensing the compound (If) or the acid addition salt thereof with an a-haloketone of formula (TH) to produce the compound of formula (TV) (iii) reducing the compound (IV) to a compound of formula (V) and (iv) reducing the compound (V) to the compound of formula (VI), wherein the reduction is carried out in the presence of" either (1 ) a hydrogen donating com pound in the presence of a hydrogen transfer catalyst or (2) ammonium formate using a hydrogenation catalyst, wherein: Rl and R2 are independently optionally substituted arylalkyl, and Hal is selected from chloro or bromo.
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