Formal synthesis of the ACE inhibitor benazepril x HCl via an asymmetric aza-Michael reaction.

نویسندگان

  • Luo-Ting Yu
  • Ji-Ling Huang
  • Ching-Yao Chang
  • Teng-Kuei Yang
چکیده

A formal enantioselective synthesis of benazepril.HCl (4), an anti- hypertensive drug, is reported. Our synthesis employed an asymmetric aza-Michael addition of L-homophenylalanine ethyl ester (LHPE, 1) to 4-(2-nitrophenyl)-4-oxo- but-2-enoic acid methyl ester (6) as the key step to prepare (2S,3'S)-2-(2-oxo-2,3,4,5- tetrahydro-1H-benzo[b]azepin-3-ylamino)-4-phenylbutyric acid ethyl ester (8), which is the key intermediate leading to benazepril x HCl (4).

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عنوان ژورنال:
  • Molecules

دوره 11 8  شماره 

صفحات  -

تاریخ انتشار 2006