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闃跨珛鍝屽攽鐨勫悎鎴愯矾绾
2015-05-10 07:08:00

闃跨珛鍝屽攽鐨勫寲瀛﹀悕7-[4-[4-(2,3-浜屾隘鑻?熀)-1-鍝屽棯鍩篯涓佹哀鍩篯-3,4-浜屾阿-2(1H)-鍠瑰晧閰?/p>

闃跨珛鍝屽攽(瀹夊緥鍑?Aripiprazole,Abilify)鏄?竴绉嶉潪鍏稿瀷鎶楃簿绁炲垎瑁傜棁鑽?墿锛屼负鍠瑰晧閰??鐢熺墿锛岄樋绔嬪搶鍞戞槸绗?竴绉嶅?宸磋兒绯荤粺绋冲畾鍓傦紝瀵圭簿绁炲垎瑁傜棁闃虫?鍜岄槾鎬х棁鐘跺潎鏈夋樉钁楃枟鏁堛?鐢ㄤ簬娌荤枟绮剧?鍒嗚?鐥囷紝鐢辨棩鏈?ぇ鍐㈠埗鑽?牚寮忎細绀剧爺鍒讹紝浜?002骞?1鏈?5鏃ヨ幏缇庡浗椋熷搧鍙婅嵂鐗╃?鐞嗗眬FDA鎵瑰噯鍦ㄧ編鍥戒笂甯傦紝鍥戒骇闃跨珛鍝屽攽鏈?鍗氭?娓?brisking, 鐢熶骇鍘傚晢锛氭垚閮藉悍寮樿嵂涓?, 濂ユ淳锛堢敓浜у巶鍟嗭細涓婃捣涓?タ鍒惰嵂鏈夐檺鍏?徃锛?鍧囧凡鎵瑰噯鍦ㄤ腑鍥戒笂甯傘?瀹夊緥鍑″湪缇庡浗鐨勯攢鍞?敱鐧炬椂缇庢柦璐靛疂璐熻矗銆傚畨寰嬪嚒鐨勪富瑕佷笓鍒╀繚鎶ゅ湪缇庡浗锛屼笖瓒呰繃鍥涘垎涔嬩笁鐨勯攢鍞?潵鑷?編鍥斤紝涓撳埄灏嗕簬2015骞?鏈堟湡婊°?

闃跨珛鍝屽攽鐨勫悎鎴愯矾绾?/strong>

浠?-缇熷熀-3锛?锛庝簩姘?2(1H)-鍠瑰晧閰?负鍘熸枡,涓?锛?锛庝簩婧翠竵鐑烽啔鍖栧緱7-(4-婧翠竵姘у熀)-3,4-浜屾阿涓?(1H)鍠瑰晧閰?紝鍐嶄笌1-(2,3-浜屾隘鑻?熀)鍝屽棯鐩愰吀鐩愮缉鍚堝緱闃跨珛鍝屽攽 (7-[4-[4-(2,3-浜屾隘鑻?熀)-1-鍝屽棯鍩篯涓佹哀鍩篯-3,4-浜屾阿-2(1H)-鍠瑰晧閰?

闃跨珛鍝屽攽鐨勫埗澶囨柟娉?/strong>

7-(4-婧翠竵姘у熀)-3,4-浜屾阿-2(1H)-鍠硅?閰?殑鍒跺?
鍦ㄥ弽搴旂摱涓?姞鍏?-缇熷熀-3,4-浜屾阿-2(1H)-鍠硅?閰?2.6 g (0.2mol)銆?,4-浜屾捍涓佺兎129.5g(0.6mol)銆?1.2%KOH姘存憾娑?50ml(0.5mol)鍜孌MF975ml,鎼呮媽涓嬪姞鐑?嚦60 ºC鍙嶅簲2h.鍔犳按1L绋?噴,姘村眰鐢ㄤ箼閰镐箼閰?300ml×2) 鎻愬彇,鍚堝苟鏈夋満灞?姘存礂,鏃犳按纭?吀閽犲共鐕?杩囨护,婊ゆ恫鍑忓帇娴撶缉鍥炴敹婧跺墏,鍓╀綑鐗╃敤寮備笝閱囬噸缁撴櫠,寰?-(4-婧翠竵姘у熀)-3,4-浜屾阿-2(1H)-鍠硅?閰?8.7g,鏀剁巼68%,mp108~110ºC.

闃跨珛鍝屽攽鐨勫悎鎴?br /> 鍦ㄥ弽搴旂摱涓?姞鍏?-(4-婧翠竵姘у熀)-3,4-浜屾阿-2(1H)-鍠硅?閰?9.8g(0.1mol)銆並I25g(0.15mol)95%涔欓唶596ml,鎼呮媽鍔犵儹鑷?0 ºC,30min鍚庡姞鍏?-2,3-浜屾隘鑻?熀鍝屽棯23.1g(0.1mol)鍜屼笁涔欒兒20ml(0.15mol),鍦?0 ºC涓嬫悈鎷?h. 瓒佺儹杩囨护,婊ゆ恫鍐峰嵈缁撴櫠,杩囨护,婊らゼ鐢ㄤ箼閱囬噸缁撴櫠涓ゆ?,骞茬嚗,寰楅樋绔嬪搶鍞?5.6g, 鏀剁巼57%,mp138.9~139.6ºC.


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