CAS: 94367-21-2; (2S,5S,8S,11S)-2-(4-Hydroxybenzyl)-8,11-Diisobutyl-5-Isopropyl-1-((4-Methyl-2-Oxo-2H-Chromen-7-yl)Amino)-1,4,7,10,13-Pentaoxo-3,6,9,12-Tetraazahexadecan-16-Oic Acid

专利信息

专利号:US-6849743-B2
优先权日:1997-08-15
标 题 :Synthesis of clasto-lactacystin β-lactone and analogs thereof
发明人：SOUCY FRANCOIS; FLAMONDON LOUIS; BEHNKE MARK; ROUSH WILLIAM
权利人:MILLENNIUM PHARM INC
摘要:The present invention is directed to an improved synthesis of clasto-lactacystin-β-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-β-lactones, and analogs thereof and their use as proteasome inhibitors.

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:US-8067616-B2
优先权日:2006-04-06
标 题 :Total synthesis of salinosporamide A and analogs thereof
发明人：LING TAOTAO; MACHERLA VENKATA RAMI REDDY; POTTS BARBARA CHRISTINE; MANAM RAMA RAO; MCARTHUR KATHERINE A
权利人:LING TAOTAO; MACHERLA VENKATA RAMI REDDY; POTTS BARBARA CHRISTINE; MANAM RAMA RAO; MCARTHUR KATHERINE A; NEREUS PHARMACEUTICALS INC
摘要:The present invention relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs from a compound of formula (V).

专利号:US-11542283-B2
优先权日:2018-05-28
标题 :Synthesis of peptide borate ester compound and use thereof
发明人：QIN YANRU
权利人:JIANGSU CHIA TAI FENGHAI PHARMACEUTICAL CO LTD
摘要:Provided are a peptide borate ester compound or a pharmaceutically acceptable salt thereof, a preparation method therefor, and pharmaceutical use thereof. The peptide borate ester compound or pharmaceutically acceptable salt thereof has a structure as shown in Formula (I), and is useful in the preparation of proteasome inhibitors to treat solid tumors and hematoma.

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-8119653-B2
优先权日:2006-07-07
标 题 :Belactosin derivatives as therapeutic agents/biological probes and their synthesis
发明人：ROMO DANIEL; CHO SUNG WOOK; SMITH JEFFREY W; RICHARDSON ROBYN D
权利人:ROMO DANIEL; CHO SUNG WOOK; SMITH JEFFREY W; RICHARDSON ROBYN D; TEXAS A & M UNIV SYS
摘要:Derivatives of belactosin and their synthesis are disclosed. In certain embodiments, compounds of the present invention exhibit anti-cancer, antiviral, antibiotic, and/or auto-immune therapeutic abilities. In general, methods of synthesis disclosed herein allow for introduction of a variety of substituents at numerous positions as well as the facile introduction of a beta-lactone ring moiety. The synthetic steps comprise, in preferred embodiments, a tandem Mukaiyama aldol lactonization reaction. Data demonstrating the utility of some of the derivatives as proteasome inhibitors is also disclosed.