专利号:US-5077408-A 优先权日:1989-09-20 标 题 :Process for the synthesis of oxazolopyridine compounds 发明人:GUILLAUMET GERALD; FLOUZAT CHRISTINE 权利人:SCIENCE ORGANISATION 摘要:Process for the synthesis of compounds of formula (I): ##STR1## their pyridinium salts and N-oxides, in which formula: the nitrogen of the pyridine ring is situated in the α-, β-, γ- or δ-position with respect to the ring junction; n R 1 represents a halogen, a substituted or unsubstituted alkyl, a substituted or unsubstituted alkoxy or a nitro, substituted or unsubstituted amino, phenyl or cyano group; n 0≦m≦2; n R 2 represents a lower alkyl or cycloalkyl group, a 5- or 6-membered heterocycle containing 1 or 2 hetero atoms, substituted or otherwise, or an aryl group ##STR2## such that: R 3 represents a halogen, a substituted or unsubstituted alkyl, a substituted or unsubstituted alkoxy or a nitro, phenyl, substituted or unsubstituted sulfonyl, cyano, thioalkyl, substituted or unsubstituted amino, substituted or unsubstituted sulfinyl, mercapto, hydroxyl or ester group, n 0≦n≦5 n employing trimethylsilyl polyphosphate (PPSE) as a cyclization agent and enabling the compounds of formula (I) to be obtained in virtually quantitative yields. The compounds of formula I have anti-inflammatory, analgesic, and antipyretic activity.
专利号:US-2009264680-A1 优先权日:2004-07-07 标题:Process for the synthesis and purification of (4-methoxybutyl) (4-trifluoromethylphenyl) methanone 发明人:CASTELLIN ANDREA; GREGORI LUCA; GONZALES TRUEBA GUADALUPE; RUBELLO ALBINO; NICOLE ANDREA 权利人:CASTELLIN ANDREA; GREGORI LUCA; GONZALES TRUEBA GUADALUPE; RUBELLO ALBINO; NICOLE ANDREA 摘要:A process for the preparation of 4-trifluoromethylvalerophenone is described. The process described is a three step process comprising the synthesis of organomagnesium specie, coupling reaction between the organomagnesium specie and trifluoromethylbenzonitrile or trifluoromethylbenzoyl chloride and preferably a purification of the product obtained in suitable reaction conditions. In the process an extraction phase of the final product is not required.
专利号:US-8778958-B2 优先权日:2008-07-10 标题 :Synthesis of metabolically stable agents for alcohol and drug abuse 发明人:CASHMAN JOHN R 权利人:CASHMAN JOHN R 摘要:The disclosed opioid-related compounds and pharmaceutical compositions thereof, are useful in a variety of applications relating to the modulation of receptors and receptor signaling within and outside the nervous system. For example, the compounds and compositions are useful in methods for the treatment of addictions and other CNS-related disorders. The disclosed compounds can be delivered or administered to a mammal including humans, alone in the form of a pharmaceutically acceptable salt or hydrolysable precursor thereof, or in the form of a pharmaceutical composition, wherein a therapeutically effective amount of a compound is mixed with suitable carriers or excipients.
专利号:US-4620009-A 优先权日:1980-03-17 标 题 :Synthesis of intermediates for tetramisole, levamisole and their derivatives 发明人:RAGHU SIVARAMAN; HOFFMANN ARTHUR K; SINGH BALWANT 权利人:CYANAMID AGRICULTURAL DE PUERT 摘要:A process for the manufacture of 1-(2-alkoxyethyl)-4-phenyl-4-imidazolin-2-ones, 1-(2-alkoxyethyl)-4-phenyl-2-imidazolidones, 1-(2-alkoxyethyl)-4-phenyl-imidazolidine-2-thiones, certain of the corresponding 1-(2-hydroxyethyl) derivatives and their 3-acylated derivatives, and certain related compounds which are all useful as intermediates in a new process for the manufacture of tetramisole, dl-2,3,5,6-tetrahydro-6-phenylimidazo-[2,1-b]thiazole, and its derivatives. The compound tetramisole is useful as an anthelmintic.
专利号:US-6509484-B2 优先权日:1993-02-05 标 题:Synthesis of taxol, taxol analogs and their intermediates with variable a-ring side chain structures and compositions thereof 发明人:SWINDELL CHARLES S; KRAUSS NANCY 权利人:NAPRO BIOTHERAPEUTICS INC 摘要:The present invention relates to chemical compounds that are useful in the production of taxanes. The chemical compounds according to the present invention have a generalized formula: n wherein R 1 is + NH 3 X − where X is deprotonated organic acid such as deprotonated trifluoroacetic acid, and wherein R 2 may be acetyl or hydrogen, and P 1 may be hydrogen or a hydroxyl protecting group, such as benzyloxymethyl.
专利号:WO-2023207268-A1 优先权日:2022-04-26 标 题:Synthesis method of plant-derived deoxycholic acid 发明人:LI CHENCHEN; QIU WENWEI; LI JIE; WEN XINYI 权利人:SHANGHAI CLICK BIOTECH CO LTD 摘要:Provided is a synthesis method for deoxycholic acid, which synthesizes deoxycholic acid from plant-derived 9-OH-BA as the starting material by means of steps of side chain oxidation reaction, Wittig or Wittig-Horner reaction, dehydration reaction, hydrogenation reaction, esterification reaction, C epoxidation reaction, carbonyl reduction reaction, hydrolysis reaction, and the like.