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A Simple and Commercially Viable Process for Improved Yields of Metopimazine, a Dopamine D2-Receptor Antagonist
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2017-04-27 00:00:00 , DOI: 10.1021/acs.oprd.7b00052 Venumanikanta Karicherla 1 , Kumar Phani 1 , Mohan Reddy Bodireddy 1 , Kumar Babu Prashanth 1 , Madhusudana Rao Gajula 1 , Kumar Pramod 1
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2017-04-27 00:00:00 , DOI: 10.1021/acs.oprd.7b00052 Venumanikanta Karicherla 1 , Kumar Phani 1 , Mohan Reddy Bodireddy 1 , Kumar Babu Prashanth 1 , Madhusudana Rao Gajula 1 , Kumar Pramod 1
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An efficient, practical, and commercially viable manufacturing process was developed with ≥99.7% purity and 31% overall yield (including four chemical reactions and one recrystallization) for an active pharmaceutical ingredient, called Metopimazine (1), an antiemetic drug used to prevent emesis during chemotherapy. The development of two in situ, one-pot methods in the present synthetic route helped to improve the overall yield of 1 (31%) compared with earlier reports (<15%). For the first time, characterization data of API (1), intermediates, and also possible impurities are presented. The key process issues and challenges were addressed effectively and achieved successfully.
中文翻译：
一种简单且商业可行的方法，可提高多巴胺D 2-受体拮抗剂美托咪嗪的收率
开发了一种有效，实用且商业上可行的制造工艺，其纯度≥99.7％，总收率31％（包括四个化学反应和一个重结晶）（称为美托咪嗪（1）），这是一种用于防止呕吐的止吐药，是一种活性药物成分。在化疗期间。与先前的报道（<15％）相比，当前合成路线中两种原位单罐方法的开发有助于提高总产量1（31％）。首次提供了API（1），中间体和可能存在的杂质的表征数据。关键流程问题和挑战得到有效解决并成功实现。
更新日期：2017-05-12
中文翻译：
一种简单且商业可行的方法，可提高多巴胺D 2-受体拮抗剂美托咪嗪的收率
开发了一种有效，实用且商业上可行的制造工艺，其纯度≥99.7％，总收率31％（包括四个化学反应和一个重结晶）（称为美托咪嗪（1）），这是一种用于防止呕吐的止吐药，是一种活性药物成分。在化疗期间。与先前的报道（<15％）相比，当前合成路线中两种原位单罐方法的开发有助于提高总产量1（31％）。首次提供了API（1），中间体和可能存在的杂质的表征数据。关键流程问题和挑战得到有效解决并成功实现。
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