L-亮氨酸置于formamide,汞体系中,用 水 作为反应溶剂,以90%的收率获得产物n-甲酰基-L-亮氨酸 参考文献:Process For Producing N-Formylleucine Of High Purity 标题:Process For Producing N-Formylleucine Of High Purity 摘要:生产n-甲酰亮氨酸的过程包括将亮氨酸与甲酰胺反应,在反应完成后,以大约0°至40oc的温度通过将反应介质与水和酸混合来沉淀n-甲酰亮氨酸,使混合物的最终ph值大约为2至3,其中所使用的水量在起始甲酰胺的重量的每部分之间大约为1.5至5部分.
专利号:US-8124794-B2 优先权日:2002-04-17 标题:Method for the asymmetric synthesis of beta-lactone compounds 发明人:SMITH JEFFREY W; AXELROD FUMIKO; KRIDEL STEVEN J; ROMO DANIEL; PUROHIT VIKRAM; MA GIL 权利人:SMITH JEFFREY W; AXELROD FUMIKO; KRIDEL STEVEN J; ROMO DANIEL; PUROHIT VIKRAM; MA GIL; SANFORD BURNHAM MED RES INST 摘要:The present invention features methods of treating a cancer in a subject by administering an effective amount of a beta-lactone to the subject. The invention also features methods of inhibiting angiogenesis in a subject by administering an effective amount of an inhibitor of fatty acid synthase to the subject. These methods can be used to treat a variety of cancers and other diseases and conditions. The invention also features methods of identifying beta-lactones and other compounds that can be used in the methods of the invention for the treatment of tumors, inhibition of angiogenesis, and the treatment of diseases and conditions that involve pathological angiogenesis. The invention also features methods of synthesizing beta-lactones and features novel beta-lactone compounds.
专利号:US-10414720-B2 优先权日:2016-09-28 标题:Process for the preparation of lacosamide 发明人:SATHE DHANANJAY G; DAS ARIJIT; Raikar Sanjay; BHAGWATKAR RAHUL; AHIRE RAMDAS 权利人:UNICHEM LAB LTD 摘要:The present invention relates to an improved process for the synthesis of (R)-Lacosamide in which free base of O-methyl-N-benzyl-D-Serinamide is not isolated before acylation. The process avoids the use of column chromatography and chiral resolution for the preparation of different stages of Lacosamide.
专利号:US-7354923-B2 优先权日:2001-08-10 标 题 :Piperazine melanocortin-specific compounds 发明人:SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH 权利人:PALATIN TECHNOLOGIES INC 摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure: n nand stereoisomer and pharmaceutically acceptable salts thereof, where X is CH 2 or Câ•?O, R 1 , R 2 , and R 3 are as described in the specification, preferably where R 3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R 3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.
专利号:US-2006258620-A1 优先权日:2002-04-17 标 题:Novel method for the asymmetric synthesis of beta-lactone compounds
专利号:WO-2005102340-A1 优先权日:2003-05-30 标题 :Piperazine melanocortin-specific compounds 发明人:SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH 权利人:PALATIN TECHNOLOGIES INC; SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH 摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure (I); and stereoisomer and pharmaceutically acceptable salts thereof, where X is CH2 or C=O, R1, R2, and R3 are as described in the specification, preferably where R3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.
专利号:JP-2009173635-A 优先权日:2000-02-04 标题:Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-2h-pyran-2-one
参考标题:Enantioselective Synthesis Of Quaternary δ4 - And δ5 -Dehydroprolines Based On A Two-Step Formal [3+2] Cycloaddition Of α-Aryl And α-Alkyl Isocyano(Thio)Acetates With Vinyl Ketones 作者:Amaiur Odriozola,Mikel Oiarbide,Claudio Palomo |发布日期:2017.9.18 摘要:Of Optically Active Quaternary δ4‐ And δ5‐dehydro Prolines Is Developed Based On The First Catalytic Enantioselective Conjugate Addition Of α‐substituted Isocyano(Thio)Acetates To Vinyl Ketones That Is General For Both α‐aryl And α‐alkyl Isocyano(Thio)Acetates. The New Tetrasubstituted C−n Stereocenter Is Formed Without The Need Of Any Metal Salt Due To A Bifunctional Tertiary Amine/squaramide Catalyst