📜氰乙酸乙酯置于溶剂黄146,硫酸二甲酯体系中,用 四氢呋喃,水 用作溶剂,以86.7%的收率获得2-氰基-2-甲基丙酸乙酯 参考文献:Synthetic Intermediate For Epothilone Derivative And Production Method Thereof 标题:Synthetic Intermediate For Epothilone Derivative And Production Method Thereof 摘要:这些化合物分别为&bgr;-酮酯化合物,&bgr;-羟基酸化合物和1,3-二醇衍生物的缩醛形式,其化学式分别为(I),(V)和(Viii),其中每个符号的定义见说明书,它们可作为一种合成中间体,用于开发作为抗肿瘤药物的依托酮衍生物.
专利号:US-2012149895-A1 优先权日:2009-04-01 标题 :Process for dimethylation of active methylene groups 发明人:JENKO BRANKO; COPAR ANTON 权利人:JENKO BRANKO; COPAR ANTON; LEK PHARMACEUTICALS 摘要:The present invention discloses a process for dimethylation of active methylene groups. Specifically, the invention discloses a process for preparing 3-amino-2,2-dimethylpropanamide. Compounds produced by the present dimethylation process such as 3-amino-2,2-dimethylpropanamide can be used as intermediates in the route of synthesis of therapeutic, prophylactic or diagnostic agent, for example aliskiren or cryptophycin. Particularly, the invention relates to embodiments further extending to processes for preparing pharmaceutical dosage form comprising said therapeutic, prophylactic or diagnostic agents. More specifically, the invention relates to the use of compounds produced by the present dimethylation process for the manufacture of therapeutic, prophylactic or diagnostic agents or for the manufacture of pharmaceutical dosage forms comprising said therapeutic, prophylactic or diagnostic agents. The processes according to the present invention can be beneficially applied for the synthesis of various active pharmaceutical ingredients, such as aliskiren or crypthophycin.
专利号:WO-2011148392-A1 优先权日:2010-05-28 标题 :Process for the preparation of (2s,4s,5s,7s)-n-(2-carbamyl-2- methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3- methoxypropoxy)phenyl]-octanamide hemifumarate and its intermediates thereof 发明人:SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; VENKAT REDDY GHOJALA; RAMA SUBBA REDDY KARAMALA; SAHADEVA REDDY MARAMREDDY 权利人:MSN LAB LTD; SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; VENKAT REDDY GHOJALA; RAMA SUBBA REDDY KARAMALA; SAHADEVA REDDY MARAMREDDY 摘要:The present invention relates to a process for the preparation of (2S,4S,5S,7S)-N-(2- Carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3-methoxy propoxy )phenyl]-octanamide compound of formula- 1 and its pharmaceutically acceptable salts thereof. Further, relates to the processes for the preparation of (R)-4-(2-(halomethyl)-3- methylbutyl)-l-methoxy-2-(3-methoxypropoxy) benzene and (R)-2-(4-methoxy-3-(3-methoxy propoxy) benzyl)-3-methyIbutan-l-ol useful intermediates in the synthesis of compound of formula- 1.
专利号:US-2007191395-A1 优先权日:2004-02-16 标题 :Heterocyclic compounds having antifungal activity 发明人:KAWAKAMI KATSUHIRO; KANAI KAZUO; FUJISAWA TETSUNORI; MORITA CHIKANORI; SUZUKI TAKASHI 权利人:KAWAKAMI KATSUHIRO; KANAI KAZUO; FUJISAWA TETSUNORI; MORITA CHIKANORI; SUZUKI TAKASHI 摘要:A compound which can specifically or selectively expresses an antifungal activity with a broad spectrum, based on the functional mechanism of 1,6-β-glucan synthesis inhibition, is provided, and an antifungal agent which comprises such a compound, a salt thereof or a solvate thereof is provided. A compound represented by the following formula (I), a salt thereof or a solvate thereof.