CAS: 134381-21-8; Epoxomicin

上下游产品

(2S,3S)-2-[[(2S,3S)-2-[acetyl(Methyl)Amino]-3-Methylpentanoyl]Amino]-N-[(2S,3R)-1-[[(2R,4S)-1-[tert-Butyl(Dimethyl)Silyl]Oxy-2-Hydroxy-2,6-Dimethyl-3-Oxoheptan-4-Yl]Amino]-3-[(2-Methylpropan-2-yl)Oxy]-1-Oxobutan-2-Yl]-3-Methylpentanamide 817204-16-3
Ac(Me)Ile2-Thr(Tbu)-Oh 817204-15-2
Ac-Meile-Ile-Oh 817204-21-0

📜N-叔丁氧羰基-N-甲基-L-异亮氨酸置于palladium On Activated Charcoal 4-二甲氨基吡啶,Sodium Hydroxide,四丁基氟化铵,氢气,Potassium Carbonate,1-羟基苯并三唑,三乙胺,N,N-二异丙基乙胺,N,N'-二环己基碳二亚胺,三氟乙酸体系中,用 四氢呋喃,甲醇,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,23.0 °C,101.33 Kpa 条件下,反应 32.0H,反应生成N-乙酰基-N-甲基-L-异亮氨酰-L-异亮氨酰-N-[(1S)-3-甲基-1-[[(2R)-2-甲基-2-环氧乙烷基]羰基]丁基]-L-苏氨酰胺
参考文献:全合成中的螺二环氧化物:Epoxomicin
标题:全合成中的螺二环氧化物:Epoxomicin
摘要:描述了螺二环氧化物官能团在全合成中的首次使用,该研究最终以有效合成有效的蛋白酶体抑制剂环氧霉素为高潮.通过氧化从丙二烯衍生的螺二环氧化物显示出顺式双取代酮及其衍生物,包括原酸酯,恶唑啉,叠氮环氧化物以及含磺酰胺,酰胺和叠氮化物的羟基酮.
Doi:10.1021/ja044563C

专利信息

专利号:US-11708341-B2
优先权日:2016-08-05
标题:Synthesis of (S)-2-amino-4-methyl-((R)-2-methyloxirane-2-yl)-pentan-1-one and pharmaceutically acceptable salts thereof
发明人：Beaver Matthew; CUI SHENG; SHI XIANGQING
权利人:AMGEN INC
摘要:The present invention provides new methods for preparing compound 5, and pharmaceutically acceptable salts thereof, of structure n nCompound 5, or a pharmaceutically acceptable salt thereof, is an important intermediate in the synthesis of carfilzomib. The invention further provides methods of making a useful manganese catalyst that may be used in the epoxidation step of the present invention.

专利号:US-2005256324-A1
优先权日:2004-05-10
标 题:Synthesis of amino acid keto-epoxides
发明人：LAIDIG GUY J; RADEL PEGGY A; SMYTH MARK S
权利人:PROTEOLIX INC
摘要:This invention relates to methods for the preparation of amino acid keto-epoxides. Specifically, allylic ketones are stereoselectively converted to the desired keto epoxides.

专利号:WO-2018100050-A1
优先权日:2016-12-01
标 题 :Process for the preparation of an intermediate for the synthesis of carfilzomib
发明人：PASTÓ AGUILÀ Mireia; ÉCIJA QUERALT MARTA
权利人:ENANTIA S L
摘要:The present invention provides a compound which is the trichloroacetic acid salt of a compound of Formula (II) wherein R is selected from the group consisting of H, CH 3- , (CH 3 ) 2 CH-, (CH 3 ) 2 CHCH 2 -, CH 3 CH 2 CH(CH 3 )-, and PhCH 2 -, and a process for its preparation. Formula (II) Also provided is a process for its preparation based on the stereoselective epoxidation of the corresponding olefin precursor and a process for the preparation of several pharmaceutically active ingredients comprising the preparation of the compound of formula (II).

专利号:US-9822145-B2
优先权日:2014-10-27
标题:Methods of making carfilzomib and intermediates thereof
发明人：KOVI RAVISHANKER; KANNAPAN JAYARAMAN; RAMU VASANTHAKUMAR G; PRASAD ALAPARTHI LAKSHMI; CHOWDARY TALLURI BHUSHAIAH; KULKARNI GAURAV; AHMED SAIYED AKEEL AHMED SHAKEEL; BOBBILI VEERABHADRA RAO; DUSANAPUDI N V RAGHAVALU; MANTRI ANAND V
权利人:APICORE US LLC
摘要:Racemization-free methods are disclosed for the synthesis of carfilzomib. Novel intermediates and methods of making carfilzomib employing fragment condensation using the novel intermediates are disclosed. Amorphous carfilzomib and methods of making same are disclosed.

专利号:EP-1756079-A2
优先权日:2004-05-17
标 题:Synthesis of amino acid keto-epoxides
发明人：LAIDIG GUY J; RADEL PEGGY A; SMYTH MARK S
权利人:PROTEOLIX INC
摘要:This invention relate to methods for the preparation of amino acid keto-epoxides according to scheme (I). Specifically, allylic ketones are stereoselectively converted to the desired keto epoxides.

专利号:US-7282491-B2
优先权日:2002-12-06
标 题 :Prokaryotic proteasomal proteases of Mycobacterium tuberculosis (MTB) as targets for antibiotic therapy
发明人：DARWIN KATERINA HERAN; NATHAN CARL F
权利人:CORNELL RES FOUNDATION INC
摘要:The present invention relates to methods of treating Mycobacterium pathogen infection in a subject that involve: inhibiting proteasomal activity in a pathogen under conditions effective to make the pathogen susceptible to antibacterial host defenses; inhibiting enzyme activity in a pathogen under conditions effective to make the pathogen susceptible to antibacterial host defenses, where the enzyme is a DNA repair enzyme or a flavin-like co-factor synthesis enzyme, or inhibiting proteasomal and enzyme activity under conditions to make the pathogen susceptible to antibacterial host defenses. The present invention also relates to methods for screening compounds that inhibit proteasomal and protease activity, DNA repair enzyme activity, or flavin-like co-factor synthesis enzyme activity, where the inhibitory compounds have an ability to sensitize bacteria to the antibacterial effects of oxidative/nitrosative stress.