文献类型：专利

英文题名：New aryl isoquinoline derivative for preventing and curing the benign tumor, cancer and diabetes

作者：CHEN K;LI B;ZENG B;ZHU W

机构：[1]UNIV EAST CHINA SCI & TECHNOLOGY;[2]UNIV SHANGHAI TCM;[3]CHINESE ACAD SCI SHANGHAI MATERIA MEDICA

申请号：CN102464615-B

公开日：2015-08-19

语种：英文

收录：DERWENT

摘要：NOVELTY - An aryl isoquinoline derivative (I) is new. USE - For preventing and curing the benign tumor, cancer and diabetes (claimed). ADVANTAGE - The compound has selectivity of tyrosine kinase and serine/threonine kinase inhibition. DETAILED DESCRIPTION - An aryl isoquinoline derivative of formula (I) is new. R1 and R2=H, hydroxyl or alkoxy;or R1+R2=methylenedioxy; R3=hydrogen, halogen or alkenyl; R4=absent, hydrogen, allyl, 1,3-dyhydroxyl, 1,3-di-tert-butyl dimethyl siloxy isopropyl or 1-methoxy-2-hydroxy ethyl;or R3+R4=-CH=CHCH2-, -CH(OH)CH(OH)CH2- or -CH(OAc)CH(OAc)-CH2-; R5=alkoxy (substituted by epoxy ethyl, alkoxy, aldehyde group or alkyl carbonyl), oxygen, alkoxy, halogenated alkoxy, or unsaturated hydrocarbon oxy group; R6 and R7=hydrogen, hydroxyl or alkoxy;or R6+R7=methylenedioxy; R8=hydrogen or halogen. The dotted line indicates double bond or single bond. The alkoxy is linear chain or branch 1-7C alkoxy. The alkenyl is linear chain or branch 2-7C alkenyl. The halogen is fluorine, chlorine, bromine or iodine. The alkyl is linear chain or branch 1-7C alkyl. The unsaturated hydrocarbon oxy group is linear chain or branch chain 2-7C alkenyl oxy or 2-7C alkynyl oxy. The alkoxy substituted by epoxy ethyl is 1-5C alkoxy substituted by epoxy ethyl. The alkoxy substituted by alkoxy is 3-7C alkoxy substituted by 1-2C alkoxy. The alkoxy substituted by aldehyde group is 3-7C alkoxy substituted by aldehyde group. The alkoxy substituted by alkyl carbonyl is 1-4C alkoxy substituted by 1-3C alkyl carbonyl. An INDEPENDENT CLAIM is included for preparation of compound (I) involves dissolving carbonyl compound of formula (III) into tetrahydrofuran, reducing temperature to be -40 degrees C, and dropping n-butyl lithium drop by drop, stirring and reacting; after that, adding the tetrahydrofuran solution of cyanide compound (II), and stirring and reacting at room temperature to form the compound (I) (where dotted line is single bond).