PFRENGLE, WALDEMAR,PACHUR, THORSTEN,NICOLA, THOMAS,DURAN, ADIL
申请号：
HK08103534.9
公开号：
HK1109405B
申请日:
2008.03.31
申请国别(地区):
HK
年份:
2014
代理人:
摘要：
Method for preparing 8-(3-aminopiperidin-1-yl)-xanthine derivatives (I) and their enantiomers and salts. Method for preparing 8-(3-aminopiperidin-1-yl)-xanthine derivatives of formula (I) and their enantiomers and salts by: (a) reacting an 8-X-xanthine (III) with 3-phthalimidopiperidine (A), or its enantiomer； (b) deprotecting the product (II)； and (c) optionally conversion to salt. X : halo or sulfonate ester, especially bromo； R 1>； : phenylcarbonylmethyl, benzyl, naphthylmethyl, pyridinylmethyl, pyrimidinylmethyl, (iso)quinolinylmethyl, quinazolinylmethyl, quinoxalinylmethyl, naphthyridinylmethyl or phenanthridinylmethyl, all optionally substituted by one or two, same or different, Ra； R 2>； : 1-3C alkyl, cyclopropyl or phenyl； R 3>； : 2-buten-1-yl, 3-methyl-2-buten-1-yl, 2-butyn-1-yl, or 2-(fluoro, chloro, bromo, iodo, methyl, trifluoromethyl or cyano)-benzyl； Ra : hydrogen, fluoro, chloro, bromo, cyano, methyl, trifluoromethyl, ethyl, phenyl, methoxy, di- or tri-fluoromethoxy, or two Ra on adjacent C atoms complete OCH 2O or OCH 2CH 2O Independent claims are also included for the following: (1) (R) and (S)-3-phthalimidopiperidine as new compounds； and (2) methods for preparing the compounds of (1). [Image] [Image] ACTIVITY : Antidiabetic； Antiarthritic； Anorectic； Osteopathic. No details of tests for these activities are given. MECHANISM OF ACTION : Inhibition of dipeptidylpeptidase IV.
