浙江化工
浙江化工
절강화공
ZHEJIANG CHEMICAL INDUSTRY
2012年
6期
25-26
,共2页
卢小逸%吴文良%董道敏%张启明
盧小逸%吳文良%董道敏%張啟明
로소일%오문량%동도민%장계명
非索非那定%关键中间体%合成
非索非那定%關鍵中間體%閤成
비색비나정%관건중간체%합성
fexofenadine%key intermediate%synthesis
以4-(4-氯丁酰基)-α,α-二甲基苯乙酸甲酯(5)为原料,与4-氰基哌啶(4)缩合,再与二苯甲酮(2)反应得到了2-[4-[4-[4-(羟基二苯甲基)-1-哌啶基]-1-氧代丁基]苯基]-2,2-二甲基乙酸甲酯(1),总收率约79%。该工艺反应条件温和,副反应少,易于操作,是一条适于工业化生产的合成路线。
以4-(4-氯丁酰基)-α,α-二甲基苯乙痠甲酯(5)為原料,與4-氰基哌啶(4)縮閤,再與二苯甲酮(2)反應得到瞭2-[4-[4-[4-(羥基二苯甲基)-1-哌啶基]-1-氧代丁基]苯基]-2,2-二甲基乙痠甲酯(1),總收率約79%。該工藝反應條件溫和,副反應少,易于操作,是一條適于工業化生產的閤成路線。
이4-(4-록정선기)-α,α-이갑기분을산갑지(5)위원료,여4-청기고정(4)축합,재여이분갑동(2)반응득도료2-[4-[4-[4-(간기이분갑기)-1-고정기]-1-양대정기]분기]-2,2-이갑기을산갑지(1),총수솔약79%。해공예반응조건온화,부반응소,역우조작,시일조괄우공업화생산적합성로선。
2-[4-[4-[4-(Hydroxydiphenylmethyl) - 1 -piperidinyl]- 1 -oxobutyl]phenyl]-2,2 -dimethylaeetic acid methyl ester was synthesized from methyl 4-(4-chloro-l-oxobutyl)-α,α-dimethylphenyl acetate with piperidine- 4-carbonitrile to give methyl 2-(4-(4-(4-cyanopiperidin-l-yl)butanoyl)phenyl)-2-methylpropanoate,which was reacted with benzophenone and with an overall yield of 79%. This method is a suitable route for industrial manufacture with advantages of mild condition, few side reaction and easy operation.