专利号:US-4219489-A 优先权日:1978-09-05 标题:Synthesis of steroids 发明人:BUNES LEONARD A; JOHNSON WILLIAM S 权利人:STANFORD LELAND JUNIOR UNIV TR 摘要:Method and compounds are provided for use in the synthesis of steroids wherein a polyolefin is provided having an initiating group having a chalcogen atom in juxtaposition to a double bond, so as to be capable of bond formation to close to form a ring and having a terminating group involving pi unsaturation (a double or triple bond) conjugated to an aromatic ring. Upon acid catalysis, sigma bonds are formed through the interaction of a carbocation formed at the carbon atom bonded to the chalcogen atom and the double bond intermediate the initiating group and the terminating group, which close to form rings of a steroid nucleus, the carbocation interacting with the pi unsaturation conjugated with the aromatic group and being captured by a nucleophile present in the acidic reaction medium. The resulting steroid product may then be modified in known ways to produce known steroids.
专利号:US-2012029226-A1 优先权日:2009-02-06 标题:Method for the synthesis of chiral alpha-aryl propionic acid derivatives 发明人:KAPTEIN BERNARDUS; VLIEG ELIAS; NOORDUIN WILLEM LIEUWE 权利人:KAPTEIN BERNARDUS; VLIEG ELIAS; NOORDUIN WILLEM LIEUWE 摘要:The present invention provides a method for the synthesis of optically pure α-aryl propionic acid derivatives comprising subjecting the corresponding racemic α-aryl propionic acid derivatives to high sheer or impact forces, such as grinding.
专利号:US-8450365-B2 优先权日:2009-05-12 标 题 :Efficient synthesis of galanthamine 发明人:MAGNUS PHILIP D; FAUBER BEN; SANE NEERAJ 权利人:MAGNUS PHILIP D; FAUBER BEN; SANE NEERAJ; UNIV TEXAS 摘要:The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.
专利号:US-10829792-B2 优先权日:2017-03-21 标 题 :Biocatalytic synthesis of strained carbocycles 发明人:CHEN KAI; HUANG XIONGYI; KAN S B JENNIFER 权利人:CALIFORNIA INST OF TECHN 摘要:Provided herein are methods for producing products containing strained carbocycles, such as cyclopropene moieties and/or bicyclobutane moieties. The methods include combining an alkyne and a carbene precursor in the presence of a heme protein, e.g., a cytochrome P450, under conditions sufficient to form the strained carbocycle. Reaction mixtures for producing strained carbocycles are also described, as well as whole-cell catalysts comprising heme proteins and variants thereof for forming cyclopropenes, bicyclobutanes, and related products.
专利号:US-6288297-B1 优先权日:1998-10-01 标 题:Process for the preparation of cyclopropylacetylene 发明人:WANG ZHE; YIN JIANGUO; FORTUNAK JOSEPH M; CAMPAGNA SILVIO 权利人:DU PONT PHARM CO 摘要:The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In the process, for example, cyclopropane carboxaldehyde is alkylated to form 1,1,1-trichloro-2-cyclopropyl-ethanol; which in turn is hydroxy protected to form 1,1,1-trichloro-2-cyclopropylethyltosylate; which in turn undergoes elimination to form cyclopropyl acetylene. This improvement provides for high conversion of inexpensive, readily available starting materials into cyclopropylacetylene, high overall yields and can be conducted on an industrial scale.
专利号:US-7553646-B2 优先权日:2005-07-28 标题 :Microbial sulfoxidation and amidation of benzhdrylsulfanyl carboxylic acids and uses thereof 发明人:OLIVO HORACIO F; OSORIO-LOZADA ANTONIO VICTOR 权利人:UNIV IOWA RES FOUND 摘要:The present invention provides novel methods for the synthesis of racemic and enantiomers of modafinil via microbial oxidation-amidation transformation. The methods include the successive oxidation-amidation of benzhydrylsulfanyl carboxylic acid to produce racemic and enantiomers of modafinil using at least one microorganism of yeast, bacteria, or fungus. Also disclosed are pharmaceutical compositions of racemic and enantiomers of modafinil along with their use in the treatment of diseases, including attention deficit hyperactivity disorder and drug addiction.
摘要:Witt, D., Science of Synthesis Knowledge Updates, (2019) 2, 291. 摘要:Belderrain, T. R.; Nicasio, M. C., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 1, 263. 摘要:Li, D.-D.; Wang, G.-W., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 375. 摘要:Dornan, L. M.; Hughes, N. L.; Muldoon, M. J., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 551. 摘要:Casano, G.; Ouari, O., Science of Synthesis, (2021) , 59.