发明名称 |
PROCESS FOR THE PREPARATION OF 2,2'-[5-(1,2,4-TRIAZOLE-1-YLMETHYL) -1,3-PHENYLENE] DI (2-METHYLPROPIONITRILE). |
摘要 |
<p>The present invention discloses a process for the preparation of Anastrozole of the formula I in high purity and in high yield. 3,5-bis(halomethyl)toluene is prepared by reacting mesitylene with N-halosuccinimide in the presence of light or dibenzoyl peroxide or azobis isobutyronitrile as a catalyst and in a chlorinated solvent. 3,5-bis(halomethyl)toluene is cyanated with metal cyanide in the presence of a catalyst and in water, organic solvent or mixture thereof at temperature of 40 to 60° C to obtain 2,2'-(5-methyl-l,3 phenylene)diacetonitrile which is further methylated with iodomethane in the presence of base and an organic solvent at temperature of 0 to 15° C to obtain 2,2'-(5-methyl-l,3-phenylene)di(2-methyl-propiononitrile). The product obtained is treated with N-halosuccinimide in the presence of a catalyst and in a chorinated solvent at temperature of 60 to 100° C to obtain 2,2'-(5-halomethyl-l,3-phenylene)di(2-methyl propionitrile) which was further treated with potassium or sodium salt 1,2,4-triazole at temperature of 20 to 50° C in dimethyl formamide to obtain crude 2,2'-[5-(lH-l,2,4-triazole-l-ylmethyl)-l,3-phenylene]di(2- methylpropionitrile). The crude product is purified by column chromatography using a stationary phase and a mobile phase followed by recrystallization with a solvent or mixture of solvents to obtain highly pure Anastrozole.</p> |
申请公布号 |
WO2007039913(A1) |
申请公布日期 |
2007.04.12 |
申请号 |
WO2005IN00332 |
申请日期 |
2005.10.05 |
申请人 |
USV LIMITED;TARUR, VENKATASUBRAMANIAN, RADHAKRISHNAN;BHISE, NANDU, BABAN;SATHE, DHANANJAY, GOVIND;CHAUDHARI, CHHAYENDRA, JANARDAN;JOSHI, MEHUL, ASHOKKUMAR |
发明人 |
TARUR, VENKATASUBRAMANIAN, RADHAKRISHNAN;BHISE, NANDU, BABAN;SATHE, DHANANJAY, GOVIND;CHAUDHARI, CHHAYENDRA, JANARDAN;JOSHI, MEHUL, ASHOKKUMAR |
分类号 |
C07D249/08;C07C17/14 |
主分类号 |
C07D249/08 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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