专利号:US-4879389-A 优先权日:1986-06-25 标题:Chiral phosphinopyrrolidine compounds and their use for asymmetric synthesis of optically active compounds 发明人:ACHIWA KAZUO 权利人:ACHIWA KAZUO 摘要:New chiral phosphinopyrrolidine compounds of the general formula: (I) or (I') wherein R1 is a hydrogen atom, -COR, -COOR, -CONHR or -SO2-R where R is an alkyl or aryl group, R2 and R3 each represents independently an aryl group which may have a substituent or substituents, and R4 and R5 each represents independently an aliphatic or cycloaliphatic hydrocarbyl group which may have a substituent or substituents, as well as the use of these compounds as ligand for a metal complex catalyst for asymmetric synthesis of optically active compounds. The new chiral phosphinopyrrolidine compounds are useful ligands which attain both of high optical yield and high reaction efficiency in catalytic asymmetric reduction.
专利号:US-11040939-B1 优先权日:2020-06-23 标 题 :N-transfer reagent and method for preparing the same and its application 发明人:CHOU HO-HSUAN; LU GUAN-HAN; HSUEH HSIAO-CHIN; HUANG TZU-CHIA 权利人:UNIV NAT CHENG KUNG 摘要:Provided are a novel N-transfer reagent and a method for preparing the same and its application. The N-transfer reagent is represented by the following Formula (I): n n n n n n n n n n The various novel N-transfer reagents of the present invention can be quickly prepared by employing different nitrobenzene precursors. The N-transfer reagents can directly convert a variety of amino compounds into diazo compounds under mild conditions. Particularly, the N-transfer reagents can facilitate the synthesis of the diazo compounds. The application of synthesizing diazo compounds of the present invention can greatly decrease the difficulty in operation, increase the safety during experiments, reduce the cost of production and the environmental pollution, and enhance the industrial value of diazo compounds.
专利号:US-12234240-B2 优先权日:2018-08-09 标 题:Substituted imidazo[5,1-d][1,2,3,5]tetrazines for the treatment of cancer 发明人:HERGENROTHER PAUL J; FAN TIMOTHY M; SVEC RILEY L 权利人:UNIV ILLINOIS 摘要:New synthetic methods to provide access to previously unexplored functionality at the C8 position of substituted imidazo[5,1-d][1,2,3,5]tetrazines of Formula I. Through synthesis and evaluation of a suite of compounds with a range of aqueous stabilities (from 0.5 to 40 hours), a predictive model for imidazotetrazine hydrolytic stability based on the Hammett constant of the C8 substituent was derived. Promising compounds were identified that possess activity against a panel of GBM cell lines, appropriate hydrolytic and metabolic stability, and brain-to-serum ratios dramatically elevated relative to TMZ, leading to lower hematological toxicity profiles and superior activity to TMZ in a mouse model of GBM.
专利号:US-5580751-A 优先权日:1990-09-14 标题:Process for the preparation of C-terminally amidated peptides 发明人:BUCHARDT OLE; BREDDAM KLAUS; HENRIKSEN DENNIS 权利人:CARLSBERG AS 摘要:A process for preparing C-terminally amidated peptides, Peptide-NH2, is presented. In a first step, a substrate component is reacted with a nucleophile component in the presence of trypsin or a carboxypeptidase using as nucleophile a compound NH2-R to form a first reaction product Peptide-NH-R. In a second step, the first reaction product is non-enzymatically chemically cleaved to form the C-terminally amidated product, Peptide-NH2. The substrate component is selected from a) peptide derivatives Peptide-X-Y, where X is an amino acid or peptide residue and Y is OH, OMe or C-terminal modification and c) C-terminally esterified peptides, Peptide-OR', where R' is alkyl, aryl, heteroaryl, or aralkyl. The nucleophile component is selected from wherein A-F and A'-E' are carbon atoms or up to two hetero atoms, Y is H, alkyl, aryl, aralkyl, oxo or carboxy, X1-X5 are H or various substituents. The cleavage may be induced by photolysis, solvolysis, reduction, rearrangement elimination, or oxidation. The process may be adapted to enzymatic synthesis and lends itself to C-terminal amidation of many types of peptides.
专利号:US-12304912-B2 优先权日:2020-07-28 标 题 :Fused bicyclic RAF inhibitors and methods for use thereof 发明人:BELFIELD ANDREW; JONES CLIFFORD DAVID; MARGATHE JEAN-FRANÇOIS; COLLETTO CHIARA 权利人:JAZZ PHARMACEUTICALS IRELAND LTD 摘要:The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.
专利号:US-7629488-B2 优先权日:2005-03-14 标 题 :Process for the preparation of opioid modulators 发明人:CAI CHAOZHONG; HE WEI 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to novel processes for the preparation of opioid modulators (agonists and antagonists) and intermediates in their synthesis. The opioid modulators are useful for the treatment and prevention of as pain and gastrointestinal disorders.
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合成参考文献
摘要:Quarterly Journal of Pharmacy & Pharmacology., 9(203), 1936 摘要:Boyd, G. V., Science of Synthesis, (2002) 11, 410. 摘要:Kantlehner, W., Science of Synthesis, (2006) 24, 418.