专利号:US-9567308-B1 优先权日:2015-07-23 标 题:Process for the synthesis of chlorzoxazone 发明人:BOGOGNA LUIGI; CICIONE LAVINIA; BAROZZA ALESSANDRO; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:Disclosed is a process for the synthesis of chlorzoxazone (1) from 4-chloro-2-aminophenol and ethyl chloroformate in the presence of a base. n n n n n n n n n n The process is particularly advantageous because it uses ethyl chloroformate instead of triphosgene, a highly dangerous reagent that releases phosgene and must be handled with extremely strict procedures to guarantee the safety of operators in industrial facilities. n Ethyl chloroformate allows the possibility of working with a number of solvents, including water. n The yield and purity of the product obtained are very high.
专利号:US-6177572-B1 优先权日:1997-08-20 标题 :Solid and liquid-phase synthesis of benzoxazoles and benzothiazoles and their use 发明人:WANG FENGJIANG 权利人:SEPRACOR INC 摘要:Methods for preparing benzoxazoles and benzothiazoles on solid supports. Substituted benzothiazoles and benzoxazoles, libraries of the compounds, and methods of using the compounds are also disclosed.
专利号:US-4005067-A 优先权日:1970-10-28 标题 :Process for the synthesis of nitrite ion-containing 1:1 complexes of cobalt and metallizable monoazo or azomethine compounds and such complexes 发明人:DORE JACKY 权利人:SANDOZ LTD 摘要:By metallization of metallizable monoazo or azomethine dyes with cobalt-donating compounds in the presence of a nitrite, especially NaNO 2 , 1:1 cobalt complexes containing a nitrite ion are obtained in a high degree of metallization which can be reacted with metallizable monoazo or azomethine dyes to give very homogeneous 2:1 cobalt complexes in a high degree of purity. This is particularly advantageous when asymmetrical 2:1 cobalt complexes are to be prepared. The process is particularly useful for the preparation of nitrite ion-containing 1:1 complexes of cobalt and a monoazo compound of the formula ##STR1## wherein X is --OH or --NHR, n wherein R is hydrogen or a substituted or unsubstituted alkyl, cycloalkyl, phenyl or naphthyl group, n Ring A is further unsubstituted or further substituted by at least one halo, nitro or optionally substituted alkyl, alkoxy or sulfamoyl substituent, and n The naphthalene ring is further unsubstituted or further substituted by at least one hydroxy, sulfamoyl or acylamino substituent.
专利号:US-2016194279-A1 优先权日:2012-12-09 标 题 :One pot process for the conversion of aroyl chlorides to acyl thioureas 发明人:CHEPURI VENKATA RAMANA; BEERAN SENTHILKUMAR 权利人:COUNCIL SCIENT IND RES 摘要:The present invention disclose an improved one pot process for synthesis of acyl thioureas of formula (I), with yield greater than 80%, from aroyl chlorides of formula (I) wherein, R′ is an aryl or a heteroarylene group substituted with one or more groups selected from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino, carboxyl, ester, halogenated hydrocarbon or an aryl or heteroaryl; R″ and R′″ are selected independently from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino or halogenated hydrocarbon.
专利号:US-2016168138-A1 优先权日:2013-07-15 标题:Process for the preparation of suvorexant and intermediates useful in the synthesis of suvorexant 发明人:IQBAL JAVED; DAHANUKAR VILAS HARESHWAR; ORUGANTI SRINIVAS; KANDAGATLA BHASKAR 权利人:REDDY S LAB LIMTED DR 摘要:A novel processes for the preparation of suvorexant (formula I), its related compounds and its intermediates that are simple, economical and commercially viable. (I)
专利号:US-7550510-B2 优先权日:2001-07-06 标 题 :Solid phase synthesis of arylretinamides 发明人:CURLEY JR ROBERT W; MERSHON SERENA M; BARNETT DEREK W; CLAGETT-DAME MARGARET; CHAPMAN JASON S 权利人:WISCONSIN ALUMNI RES FOUND 摘要:A solid phase synthetic method for preparing arylretinamides is provided. The method comprises reacting hexachloroacetone with a solvent-suspended resin-bound triphenylphosphine to provide a suspension comprising an activated chlorinating reagent; reacting retinoic acid with the activated chlorinating reagent to provide retinoyl chloride; adding pyridine and a select arylamine to the resulting mixture; and stirring the resulting mixture for a time and at a temperature sufficient for the select arylamine to react with the retinoyl chloride and provide the arylretinamide. Also provided, are select arylretinamides that can be prepared by the present method, and methods of using such arylretinamides to induce apoptosis in cancer cells.