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N-Boc-反式-4-羟基-L-脯氨酸甲酯置于对硝基苯甲磺酰氟,1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,用 甲苯 用作溶剂,化学反应生成(2S,4S)-N-Boc-顺式-4-氟-L-脯氨酸
参考文献:新型 β-内酰胺酶抑制剂 Wck 6395 的工艺开发和放大
标题:新型 β-内酰胺酶抑制剂 Wck 6395 的工艺开发和放大
摘要:描述了新型 β-内酰胺酶抑制剂 Wck 6395 的初始工艺开发.所有关键中间体很容易通过结晶或沉淀分离,以消除相关杂质.假设了七种可能的工艺相关杂质,并实施了初始控制策略.此外,还确定并改进了工艺参数以减少或避免这些杂质.通过先验知识和实验优化每个步骤的参数,以提高 Wck 6395 的产量和所需质量,以支持毒理学研究.改进后的工艺有效减少了有害试剂的使用,在千克规模上稳健,在中试规模上进行了展示,随后作为商业路线开发的基础.
Doi:10.1021/acs.Oprd.2C00349

专利信息

专利号:US-7179918-B2
优先权日:2001-06-11
标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
发明人：CANAN KOCH STACIE S; ALEXANDER THERESE N; BURKE BENJAMIN J; JEWELL TANYA M; KUCERA DAVID J; LINTON MARIA ANGELICA; MITCHELL JR LENNERT J; REICH SIEGFRIED H; SKALITZKY DONALD J; TATLOCK JOHN H; VARNEY MICHAEL D; VIRGIL SCOTT C; WEBBER STEPHEN E; WORLAND STEPHEN T; BARVIAN MARK; BOLTON GARY; BOYER JR FREDERICK EARL; MACHAK JEFFREY J; HOLLER TOD; MURPHY SEAN T; MELNICK MICHAEL; JOSYULA VARA PRASAD
权利人:AGOURON PHARMA
摘要:Compounds of the formula: n nwhere the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.

专利号:US-7169932-B2
优先权日:2001-06-11
标题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses, material for their synthesis
发明人：KUCERA DAVID JOHN; SCOTT ROBERT WILLIAM
权利人:PFIZER
摘要:Compounds of the formula: n nwhere the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.

专利号:US-7094909-B2
优先权日:2001-06-11
标 题 :HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
发明人：KUCERA DAVID JOHN; SCOTT ROBERT WILLIAM
权利人:AGOURON PHARMA
摘要:The present invention concerns processes for preparing compounds of formula (I-H), or a prodrug, pharmaceutically active metabolite, or pharmaceutically active salt or solvate thereof, n nwhich are useful as inhibitors of the HIV protease enzyme.