STEREOSELECTIVE REDUCTION FOR 2- OR 3-SUBSTITUTED-4- PIPERIDONE
申请(专利)号:
JP19840046628
申请日期:
1984-03-13
公开/公告号:
JPS59176254A
公开/公告日期:
1984-10-05
申请(专利权)人:
HEKISUTO RUSERU PHARM INC
摘要:
A stereoselective reduction of 2- or 3-substituted 4- piperidones of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl or benzyl and R.sub.2 is methyl or ethyl, to the di-equatorial isomer of the corresponding 4-piperidinol is described. Said reduction is conducted by use of sodium borohydride in a protic solvent medium at a temperature substantially lower than ambient temperature in the presence of an effective amount of an inorganic acid. Under favorable reaction conditions, the stereoselectivity of the reduction is so high that simple crystallization of the reaction product affords the pure isomer in a commercially acceptable and advantageous process.
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