专利号:US-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
专利号:US-2025034607-A1 优先权日:2021-12-03 标题 :Process of Synthesizing (R)-3-aminobutan-1-ol 发明人:BOBKO MARK; FUERST DOUGLAS; MORGAN CHRISTOPHER 权利人:VIIV HEALTHCARE CO 摘要:The present invention relates to an aminotransaminase useful in the synthesis of (R)-3-aminobutan-1-ol (RABO). The present invention also provides a process of preparing (R)-3-aminobutan-1-ol (RABO) with the disclosed aminotransaminase.
专利号:US-9365587-B2 优先权日:2008-12-11 标 题:Synthesis of carbamoylpyridone HIV integrase inhibitors and intermediates 发明人:YOSHIDA HIROSHI; TAODA YOSHIYUKI; JOHNS BRIAN ALVIN; KAWASUJI TAKASHI; NAGAMATSU DAIKI 权利人:SHIONOGI & CO; VIIV HEALTHCARE CO 摘要:The invention is a process for the preparation of a compound of the following formula (I): n nwherein R is —CHO, —CH(OH) 2 or —CH(OH)(OR 4 ); P 1 is H or a hydroxyl protecting group; P 3 is H or a carboxy protecting group; R 3 is H, halogen, hydroxy, optionally substituted lower alkyl, optionally substituted cycloalkyl, etc.; R x is H, halogen or R 2 —X—NR 1 —C(O)—; etc. as defined in the specification. The compounds are useful as intermediates in synthesizing compounds having HIV integrase inhibitory activity.
专利号:WO-2015019310-A1 优先权日:2013-08-07 标 题 :Process for the preparation of dolute-gravir and intermediates thereof 发明人:DANDALA RAMESH; VELLANKI SIVA RAM PRASAD; NADELLA MADHU MURTHY; BALUSU PHANI KUMAR 权利人:MYLAN LAB LTD 摘要:The present disclosure relates to processes for the preparation of dolutegravir or of its pharmaceutically acceptable salts. The present disclosure also provides intermediates useful in the synthesis of dolutegravir.
专利号:US-11248005-B2 优先权日:2019-07-08 标 题 :Process for preparation of intermediates used for the synthesis of HIV integrase inhibitor 发明人:JADHAV HARISHCHANDRA SAMBHAJI; SHRIVASTAVA DHANANJAI; AHER UMESH PARASHARAM; DEOKAR SHARAD CHANDRABHAN; NALE DEEPAK BABASAHEB; HONRAO SURYAKANT TUKARAM; SINGH GIRIJ PAL 权利人:LUPIN LTD 摘要:Provided herein is a process for the intermediates used for preparation of HIV Integrase Inhibitor such as Bictegravir, Dolutegravir, Cabotegravir or their pharmaceutically acceptable salts.
专利号:US-8754214-B2 优先权日:2008-12-11 标题 :Synthesis of carbamoylpyridone HIV integrase inhibitors and intermediates
摘要:Shi, Y.; Cole-Hamilton, D. J.; Kamer, P. C. J., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 2, 200. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026).