基本信息:
- 专利标题： A PROCESS FOR THE PREPARATION OF ANHYDROUS POLYMORPHIC FORM OF OLANZAPINE
- 专利标题（中）：制备OLANZAPINE无定形多形态的方法
- 申请号：PCT/IN2006/000142 申请日：2006-04-25
- 公开(公告)号：WO2007102167A1 公开(公告)日：2007-09-13
- 发明人： ALLA, Venkat, Reddy , VYAKARANAM, Kameswara, Rao , SIRIGIRI, Aruna, Kumari , BODAPATI, Srinivas, Reddy , BILLA, Ranadheer, Reddy , ALLA, Raghumitra
- 申请人： LEE PHARMA LIMITED , ALLA, Venkat, Reddy , VYAKARANAM, Kameswara, Rao , SIRIGIRI, Aruna, Kumari , BODAPATI, Srinivas, Reddy , BILLA, Ranadheer, Reddy , ALLA, Raghumitra
- 申请人地址： Flat No. 401/A, Saidatta Apartments, Srinivasa Nagar Colony (East), Ameerpet, Hyderabad 500 038 IN
- 专利权人： LEE PHARMA LIMITED,ALLA, Venkat, Reddy,VYAKARANAM, Kameswara, Rao,SIRIGIRI, Aruna, Kumari,BODAPATI, Srinivas, Reddy,BILLA, Ranadheer, Reddy,ALLA, Raghumitra
- 当前专利权人： LEE PHARMA LIMITED,ALLA, Venkat, Reddy,VYAKARANAM, Kameswara, Rao,SIRIGIRI, Aruna, Kumari,BODAPATI, Srinivas, Reddy,BILLA, Ranadheer, Reddy,ALLA, Raghumitra
- 当前专利权人地址： Flat No. 401/A, Saidatta Apartments, Srinivasa Nagar Colony (East), Ameerpet, Hyderabad 500 038 IN
- 代理机构： VISHWANATH, Ramesh, Babu
- 优先权： IN390/CHE/2006 20060306
- 主分类号： C07D495/04
- IPC分类号： C07D495/04
摘要：
Malononitrile is reacted with Propionaldehyde in presence of Sulphur Powder and Triethylamine in N,N-dimethlyformamide to give 5-Amino4- Cyano-2 -Methyl Thiophene. 2-fluoronitrobenzene is condensed with 5- Amino-4-Cyano-2-Methyl Thiophene in Isopropyl alcohol and Potassium Hydroxide powder give 4-cyano-2-methyl-1-(2-nitrophenyl amino) Thiophene. Reduction of 4-cyano-2-methyl-1-(2-nitrophenyl amino) Thiophene with Stannous Chloride and Hydrochloric acid in Isopropyl; Alcohol and followed by cyclization to get 4-Amino-2-Methyl-10H- Thieno [2,3,-b][1,5] Benzodiazepine Condensation of 4-amino-2-methyF10H-Thieno [2,3,-b][1,5] Benzodiazepine and N-methyl Piperazine in presence of Dimethyl Sulphoxide and Toluene gives Olanzapine Technical grade, in anhydrous form. Treatment of anhydrous technical Olanzapine with acetone followed by subsequent precipitation with an anti solvent gave anhydrous OLANZAPINE of Form-II.
摘要（中）：
在N，N-二甲基甲酰胺中，丙磺酸与硫醛粉末和三乙胺存在下与丙醛反应得到5-氨基-4-氰基-2-甲基噻吩。 2-氟硝基苯与异丙醇中的5-氨基-4-氰基-2-甲基噻吩缩合，氢氧化钾粉末得到4-氰基-2-甲基-1-（2-硝基苯基氨基）噻吩。 用异丙基氯化亚锡和盐酸还原4-氰基-2-甲基-1-（2-硝基苯基氨基）噻吩; 醇，然后环化，得到4-氨基-2-甲基-1H-咪唑并[2,3-b]的4-氨基-2-甲基-10H-噻吩并[2,3，b] [1,5]苯并二氮杂 ] [1,5]苯并二氮杂和N-甲基哌嗪在二甲基亚砜和甲苯存在下，得到无水形式的奥氮平技术级。 用丙酮处理无水技术的奥氮平，随后用抗溶剂沉淀，得到无规O型片II型。
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D495/00 | 杂环化合物，在稠环系中至少有1个杂环具有硫原子作为仅有的杂环原子 |
| --------C07D495/02 | .在稠环系中含有两个杂环 |
| ----------C07D495/04 | ..邻位稠合系 |