CAS: 1509-92-8; N-Acetyl-D-Methionine

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65-82-7 1115-47-5 35671-83-1

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CAS号60-35-5 乙酰胺 | CAS号3268-49-3 3-甲硫基丙醛 | CAS号201230-82-2 carbon monoxide | CAS号55585-92-7 N-acetyl-DL-hom... | CAS号1115-47-5 N-乙酰-DL-蛋氨酸 | CAS号21691-49-6 D-蛋氨酸甲酯 | CAS号10332-17-9 L-Methionine, m... | CAS号348-67-4 D-蛋氨酸 | CAS号108-24-7 乙酸酐 | CAS号348-67-4 D-蛋氨酸

N-乙酰-Dl-蛋氨酸 反应生成N-乙酰-D-蛋氨酸
参考文献:Studies On Acylase Activity And Microorganisms. Xix Optical Resolution Of Threonine,Lysine,Tryptophan,And Methionine By Acylase Of Soil Bacteria
标题:Studies On Acylase Activity And Microorganisms. Xix Optical Resolution Of Threonine,Lysine,Tryptophan,And Methionine By Acylase Of Soil Bacteria
摘要:通过使用含有氨基酸n-酰基衍生物作为唯一碳源的合成培养基,分离出15株能够不对称水解n-苯甲酰-Dl-苏氨酸,2,6-二n-苯甲酰-Dl-赖氨酸,N-乙酰-Dl-赖氨酸,N-乙酰-Dl-色氨酸或n-乙酰-Dl-蛋氨酸的土壤细菌(见表i).N-苯甲酰-Dl-苏氨酸在kt 218,Kt 229和kt 83的酰化酶作用下不对称水解为l-苏氨酸,N-苯甲酰-D-苏氨酸和苯甲酸,而2,6-二n-苯甲酰-Dl-赖氨酸则在kt 218和kt 229的作用下水解为6-N-苯甲酰-L-赖氨酸,2,6-二n-苯甲酰-D-赖氨酸和苯甲酸.Kt 241和kt 224则分别将n-乙酰-Dl-色氨酸和n-乙酰-Dl-蛋氨酸不对称水解为l-色氨酸和n-乙酰-D-色氨酸以及l-蛋氨酸和n-乙酰-D-蛋氨酸.观测到n-乙酰-D-色氨酸和n-乙酰-D-蛋氨酸被若干株土壤细菌(如kt 229,Kt 83,Kt 222等)水解.值得注意的是,N-乙酰-L-蛋氨酸比n-乙酰-L-色氨酸更容易被kt 224或kt 218水解,而后者则更容易被kt 241水解.此外,L-蛋氨酸的n-乙酰衍生物比n-苯甲酰衍生物更容易被kt 224或kt 241水解,而后者则更容易被kt 218水解.
Doi:10.1248/cpb.10.1146

专利信息

专利号:US-11548898-B2
优先权日:2017-07-06
标题 :Synthesis of halichondrins
发明人：KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI
权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD
摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).

专利号:US-2006287520-A1
优先权日:2005-05-16
标 题 :Synthesis of salinosporamide A and analogues thereof
发明人：DANISHEFSKY SAMUEL J; ENDO ATSUSHI
权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI
摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.

专利号:US-7910623-B2
优先权日:2005-07-22
标 题 :Synthesis of scabronines and analogues thereof
发明人：DANISHEFSKY SAMUEL J; WATERS STEPHEN P
权利人:SLOAN KETTERING INST CANCER
摘要:A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.

专利号:WO-2012047907-A9
优先权日:2010-10-04
标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto
发明人：MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN
权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN
摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.

专利号:US-11220513-B2
优先权日:2015-04-30
标题:Chromium-mediated coupling and application to the synthesis of halichondrins
发明人：KISHI YOSHITO; YAN WUMING; LI JINGWEI; LI ZHANJIE; YAHATA KENZO
权利人:HARVARD COLLEGE
摘要:The present invention provides unified synthesis of the C1-C19 building blocks of halichondrins and analogs thereof using selective coupling of poly-halogenated nucleophiles in chromium-mediated coupling reactions. The present invention also provides a practical and efficient synthesis of C20-C38 building blocks of halichondrins and analogs thereof. Also provided herein are general methods of selective activation and coupling of poly-halogenated analogs with an aldehyde. The provided coupling reactions are selective for halo-enone and halo-acetylenic ketal over vinyl halide and halide attached to a sp hybridized carbon. The provided efficient selective coupling reactions can allow easy access to the C1-C19 building blocks and C20-C38 building blocks of halichondrins and analogs thereof with limited or no purification or separation of the intermediates.

专利号:US-9688644-B2
优先权日:2009-04-30
标 题 :Synthesis of Tetracyclines and intermediates thereto
发明人：MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M
权利人:HARVARD COLLEGE
摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.