专利号:US-11667658-B2 优先权日:2021-06-30 标 题:Chemical synthesis of the organoarsenical antibiotic arsinothricin 发明人:ROSEN BARRY P; YOSHINAGA MASAFUMI; WNUK STANISLAW F; HOWLADER MD ABU HASAN; SUZOL SK MD SAZZAD HOSSAIN 权利人:ROSEN BARRY P; YOSHINAGA MASAFUMI; WNUK STANISLAW F; HOWLADER MD ABU HASAN; SUZOL SK MD SAZZAD HOSSAIN; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:The subject invention provides methods for the chemical synthesis of racemic arsinothricin (D,L-AST), the novel organoarsenical antibiotic. One is by condensation of the 2-chloroethyl(methyl)arsinic acid with acetamidomalonate, and the second involves reduction of the N-acetyl-protected derivative of hydroxyarsinothricin (AST-OH) and subsequent methylation of the resulting sodium salt of trivalent arsenic intermediate with methyl iodide. The enzyme AST N-acetyltransferase (ArsN1) was utilized to purify L-AST from racemic AST. This expedient chemical synthesis of AST provides a source of this novel antibiotic for future drug development.
专利号:US-11466050-B2 优先权日:2014-09-29 标 题 :Method for peptide synthesis and apparatus for carrying out a method for solid phase synthesis of peptides 发明人:KNAUER SASCHA; ROESE TOBIAS MICHAEL LOUIS; AVRUTINA OLGA; KOLMAR HARALD; UTH CHRISTINA 权利人:SULFOTOOLS GMBH 摘要:The invention relates to a method for peptide synthesis, wherein said method comprises the steps of reacting a first amino acid or a first peptide with an α-amine protected second amino acid in a solvent selected from the group consisting of water, alcohol, and a mixture of water and alcohol, and removing the α-amine protecting group with a deprotecting solution. The invention further relates to protective agents, their use and an apparatus for carrying out a method for solid phase synthesis of peptides.
专利号:US-6177564-B1 优先权日:1998-09-11 标题:Process for the synthesis of N-benzyl-3-(4-fluorophenyl)-1-4-oxazin-2-one 发明人:NELSON TODD D; BHUPATHY MAHADEVAN 权利人:MERCK & CO INC 摘要:The present invention is concerned with a novel process for the preparation of N-benzyl-3-(4-fluorophenyl)-1,4-oxazin-2-one of the formula:This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity, in particular, as substance P (neurokinin-1) receptor antagonists.
专利号:US-6159673-A 优先权日:1996-07-17 标 题:Oxonol compound, light-sensitive material and process for the synthesis of oxonol compound 发明人:NISHIGAKI JUNJI; DEGUCHI YASUAKI 权利人:FUJI PHOTO FILM CO LTD 摘要:An oxonol compound is represented by the following formula (I): in which Z is an atomic group that forms a cyclic amide ring; each of W1 and W2 independently is an atomic group that forms an acidic nucleus ring; and M is a cation. Other oxonol compounds, a light-sensitive material containing an oxonol compound and a process for the synthesis of an oxonol compound are also disclosed.
专利号:US-7423169-B2 优先权日:2001-06-11 标 题:Methods for synthesis of acyloxyalkyl derivatives of GABA analogs 发明人:RAILLARD STEPHEN P; ZHOU CINDY X; YAO FENMEI; MANTHATI SURESH KUMAR; XIANG JIA-NING; GALLOP MARK A 权利人:XENOPORT INC 摘要:The synthesis of 1-(acyloxy)-alkyl carbamates of GABA analogs from 1-haloalkyl carbamates of GABA analogs are described. Also described are new 1-haloalkyl carbamates of GABA analogs.
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.