WO2016037588A3 - 用于合成抗艾滋病药物增强剂cobicistat的中间体 - Google Patents

用于合成抗艾滋病药物增强剂cobicistat的中间体 Download PDF

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Publication number
WO2016037588A3
WO2016037588A3 PCT/CN2015/089406 CN2015089406W WO2016037588A3 WO 2016037588 A3 WO2016037588 A3 WO 2016037588A3 CN 2015089406 W CN2015089406 W CN 2015089406W WO 2016037588 A3 WO2016037588 A3 WO 2016037588A3
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WO
WIPO (PCT)
Prior art keywords
cobicistat
synthesis
aids drug
drug enhancer
disclosed
Prior art date
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PCT/CN2015/089406
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English (en)
French (fr)
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WO2016037588A2 (zh
Inventor
李昌龙
楼科侠
喻立煌
徐帅
张达
Original Assignee
宁波九胜创新医药科技有限公司
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Publication of WO2016037588A2 publication Critical patent/WO2016037588A2/zh
Publication of WO2016037588A3 publication Critical patent/WO2016037588A3/zh

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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

提供一种用于合成抗艾滋病药物增强剂cobicistat的中间体化合物I及其合成方法。还提供用该化合物I合成 (2R, 5R)-1, 6-二苯基-2, 5-己二胺的方法，该方法步骤短、条件简单易操作，生产成本低，且产品纯度高。
PCT/CN2015/089406 2014-09-12 2015-09-11 用于合成抗艾滋病药物增强剂cobicistat的新中间体 WO2016037588A2 (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201410466139.5 2014-09-12
CN201410466139.5A CN104193643B (zh) 2014-09-12 2014-09-12 用于合成抗艾滋病药物增强剂cobicistat的中间体

Publications (2)

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WO2016037588A2 WO2016037588A2 (zh) 2016-03-17
WO2016037588A3 true WO2016037588A3 (zh) 2016-05-26

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PCT/CN2015/089406 WO2016037588A2 (zh) 2014-09-12 2015-09-11 用于合成抗艾滋病药物增强剂cobicistat的新中间体

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CN (1) CN104193643B (zh)
WO (1) WO2016037588A2 (zh)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104193643B (zh) * 2014-09-12 2016-02-10 宁波九胜创新医药科技有限公司 用于合成抗艾滋病药物增强剂cobicistat的中间体
CN105017082B (zh) * 2015-07-31 2017-09-19 上海皓元医药股份有限公司 一种心衰药Entresto 关键中间体(R)‑叔丁基 (1‑([1,1`‑联苯]‑4‑基)‑3‑羟基丙烷‑2‑基)氨基甲酸酯的制备方法
CN109912426B (zh) * 2017-12-13 2023-01-13 上海奥博生物医药股份有限公司 用于合成抗艾滋病药物增强剂可比司他(cobicistant)的中间体

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012045007A1 (en) * 2010-10-01 2012-04-05 Gilead Sciences, Inc. Method of preparation of (4 - {4 -acetylamino- 2 - [3- ( 2 - isopropyl - thiazol - 4 - ylmethyl) - 3 -methyl - ureido] - butyryl amino} -1 -benzyl- 5 -phenyl- pentyl) -carbamic acid thiazol - 5 - ylmethyl ester
CN102438982A (zh) * 2009-04-03 2012-05-02 吉里德科学公司 用于制备细胞色素p450单加氧酶抑制剂的方法和所涉及的中间体
WO2013116715A1 (en) * 2012-02-03 2013-08-08 Gilead Sciences, Inc. Methods and intermediates for preparing pharmaceutical agents
US20140051888A1 (en) * 2012-08-20 2014-02-20 Ampac Fine Chemicals Llc Novel stereoisomeric mixtures, synthesis and uses thereof
CN104193643A (zh) * 2014-09-12 2014-12-10 宁波九胜创新医药科技有限公司 用于合成抗艾滋病药物增强剂cobicistat的新中间体

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102438982A (zh) * 2009-04-03 2012-05-02 吉里德科学公司 用于制备细胞色素p450单加氧酶抑制剂的方法和所涉及的中间体
WO2012045007A1 (en) * 2010-10-01 2012-04-05 Gilead Sciences, Inc. Method of preparation of (4 - {4 -acetylamino- 2 - [3- ( 2 - isopropyl - thiazol - 4 - ylmethyl) - 3 -methyl - ureido] - butyryl amino} -1 -benzyl- 5 -phenyl- pentyl) -carbamic acid thiazol - 5 - ylmethyl ester
WO2013116715A1 (en) * 2012-02-03 2013-08-08 Gilead Sciences, Inc. Methods and intermediates for preparing pharmaceutical agents
US20140051888A1 (en) * 2012-08-20 2014-02-20 Ampac Fine Chemicals Llc Novel stereoisomeric mixtures, synthesis and uses thereof
CN104193643A (zh) * 2014-09-12 2014-12-10 宁波九胜创新医药科技有限公司 用于合成抗艾滋病药物增强剂cobicistat的新中间体

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
XU, LIANHONG ET AL.: "A Novel and Efficient Synthesis of Chiral C2-Symmetric 1, 4-Diamines", TETRAHEDRON LETTERS, vol. 50, no. 5, 24 November 2008 (2008-11-24), pages 552 - 554, XP025799917, DOI: doi:10.1016/j.tetlet.2008.11.071 *
XU, LIANHONG ET AL.: "Cobicistat (GS-9350): A Potent and Selective Inhibitor of Human CYP3A as a Novel Pharmacoenhancer", ACS MEDICINAL CHEMISTRY LETTERS, vol. 1, no. 5, 17 May 2010 (2010-05-17), pages 209 - 213, XP009156835, DOI: doi:10.1021/ml1000257 *

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CN104193643B (zh) 2016-02-10
CN104193643A (zh) 2014-12-10
WO2016037588A2 (zh) 2016-03-17

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