CAS: 169280-56-2; 4-Amino-N-((2R,3S)-3-Amino-2-Hydroxy-4-Phenylbutyl)-N-Isobutylbenzenesulfonamide

上下游产品

2R-Hydroxy-3-[[(4-Aminophenyl)Sulfonyl](2-Methylpropyl)Amino]-1S-(Phenylmethyl)-Propylamine
N-((2R,3S)-3-Amino-2-Hydroxy-4-Phenylbutyl)-N-Isobutyl-4-Nitrobenzenesulfonamide 251105-80-3
(2R,3R)-3-Azido-4-Phenylbutane-1,2-Diol
[(1S,2R)-1-苄基-2-羟基-3-[异丁基-[(4-氨基苯基)磺酰基]氨基] 丙基]氨基甲酸叔丁酯 3-S-(N-Tert-Butyloxyformamido)-[2R-Hydroxy-1-[(4-Aminophenylsulfonyl)(2-Methylpropyl)]Amino]-4-Phenylbutane 183004-94-6
1-Benzyl-2-Hydroxy-3-[isobutyl-(4-Acetylaminobenzenesulfonylamino)Propyl]Carbamic Acid Tert-Butyl Ester 160230-47-7
[(1S,2R)-1-苄基-2-羟基-3-[异丁基[(4-硝基苯基)磺酰]氨基]丙基]氨基甲酸叔丁酯 [(1S,2R)-3-[(4-Nitrophenylsulfonyl)(2-Methylpropyl)Amino]-2-Hydroxy-1-(Phenylmethyl)Propyl]Carbamic Acid Tert-Butyl Ester 191226-98-9
氨甲酸,[(1S,2R)-2-羟基-3-[(2-甲基丙基)[(4-硝基苯基)磺酰]氨基]-1-(苯基甲基)丙基]-,苯基甲基酯 3-S-(N-Benzyloxyformamido)-[2R-Hydroxy-1-[(2-Methylpropyl)(4-Nitrophenylsulfonyl)]Amino]-4-Phenylbutane 159005-59-1
N-(3-二苄基氨基-2-羟基-4-苯基丁基)-N-异丁基-4-硝基苯磺酰胺 N-(3-Dibenzylamino-2-Hydroxy-4-Phenylbutyl)-N-Isobutyl-4-Nitrobenzenesulfonamide 244641-42-7

[(1S,2R)-1-苄基-1-苄氧羰基氨基-2-羟基-4-N-异丁基氨基丙烷置于palladium On Activated Charcoal 氢气,三乙胺体系中,用 二氯甲烷,乙酸乙酯 用作溶剂,化学反应生成4-氨基-N-[(2R,3S)-3-氨基-2-羟基-4-苯丁基]-N-异丁基苯磺酰胺
参考文献:Discovery Of Novel Benzothiazolesulfonamides As Potent Inhibitors Of Hiv-1 Protease
标题:Discovery Of Novel Benzothiazolesulfonamides As Potent Inhibitors Of Hiv-1 Protease
摘要:The Human Immunodeficiency Virus (Hiv) Has Been Shown To Be The Causative Agent For Aids. The Hiv Virus Encodes For A Unique Aspartyl Protease That Is Essential For The Production Of Enzymes And Proteins In The Final Stages Of Maturation. Protease Inhibitors Have Been Useful In Combating The Disease. The Inhibitors Incorporate A Variety Of Isosteres Including The Hydroxy-Ethylurea At The Protease Cleavage Site. We Have Shown That The Replacement Of T-Butylurea Moiety By Benzothiazolesulfonamide Provided Inhibitors With Improved Potency And Antiviral Activities. Some Of The Compounds Have Shown Good Oral Bioavailability And Half-Life In Rats. The Synthesis Of Benzothiazole Derivatives Led Us To Explore Other Heterocycles. During The Course Of Our Studies. We Also Developed An Efficient Synthesis Of Benzothiazole-6-Sulfonic Acid Via A Two-Step Procedure Starting From Sulfanilamide. (C) 2003 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmc.2003.07.001

专利信息

专利号:US-9233943-B2
优先权日:2012-01-10
标题:Process for synthesis of syn azido epdxide and its use as intermediate for the synthesis of amprenavir and saquinavir
发明人：GADAKH SUNITA KHANDERAO; REKULA REDDY SANTHOSH; SUDALAI ARUMUGAM
权利人:COUNCIL SCIENT IND RES
摘要:A novel synthetic route to the syn-azido epoxide of formula 5 includes cobalt-catalyzed hydrolytic kinetic resolution of a racemic mixture of the azido-epoxide. Reaction steps include subjecting an allylic alcohol to epoxidation with mCPBA to obtain a racemic epoxy alcohol; ring opening the epoxy alcohol with azide anion to obtain an anti-azido alcohol, which can then be selectively tosylated at the primary alcohol; treating the tosylate with base to obtain the racemic azido-epoxide; and subjecting the racemic azido-epoxide to cobalt-catalyzed hydrolytic kinetic resolution to obtain the syn-azido epoxide of formula 5. The compound of formula 5 may be used as a common intermediate for the asymmetric synthesis of HIV protease inhibitors, such as Amprenavir, Fosamprenavir, Saquinavir, and formal synthesis of Darunavir and Palinavir.

专利号:US-2015011782-A1
优先权日:2012-01-10
标 题 :Process for synthesis of syn azido epoxide and its use as intermediate for the synthesis of amprenavir & saquinavir

专利号:US-6140505-A
优先权日:1995-03-10
标 题:Synthesis of benzo fused heterocyclic sulfonyl chlorides

专利号:US-2010168422-A1
优先权日:2008-12-30
标 题:Methods and intermediates useful in the synthesis of hexahydrofuro [2,3-b]furan-3-ol
发明人：CHEN WEIPING
权利人:CHEN WEIPING
摘要:Provided herein are compounds and methods useful for preparing hexahydrofuro[2,3-b]furan-3-ol. Hexahydrofuro[2,3-b]furan-3-ol can be efficiently synthesized in four steps from readily available starting materials.

专利号:WO-2010075887-A1
优先权日:2008-12-30
标题:Methods and intermediates useful in the synthesis of hexahydrofuro[2,3-b]furan-3-ol
发明人：CHEN WEIPING
权利人:OXYRANE UK LTD; CHEN WEIPING
摘要:Provided herein are compounds and methods useful for preparing hexahydrofuro[2,3-b]furan-3-ol. Hexahydrofuro[2,3-b]furan-3-ol can be efficiently synthesized in four steps from readily available starting materials.