42839-54-3 = 6339-87-3 + 527-72-0 + 5813-89-8 + 79-84-5 反应条件:1.1 Reagents: Sulfuric Acid Solvents: Butyl Ether,Water; 30 Min,40 °C 标题:Three Step,One-Pot Process To Prepare Thiophene-2-Carbonyl Chloride (Tcc),A Key Raw Material In The Manufacture Of Tioxazafen (Nemastrike) 作者:Walker,Daniel P.; Et Al 参考文献:Tetrahedron Letters 日期:2019 卷标:60(12) 页码:834-838]
1189-71-5 = 6339-87-3 + 527-72-0 + 5813-89-8 + 79-84-5 反应条件:1.1 Solvents: Butyl Ether; 2 H,50 °C2.1 Reagents: Sulfuric Acid Solvents: Butyl Ether,Water; 30 Min,40 °C 标题:Three Step,One-Pot Process To Prepare Thiophene-2-Carbonyl Chloride (Tcc),A Key Raw Material In The Manufacture Of Tioxazafen (Nemastrike) 作者:Walker,Daniel P.; Et Al 参考文献:Tetrahedron Letters 日期:2019 卷标:60(12) 页码:834-838
Thiophene-2-Sulfonyl Azide置于碲化氢,Sodium Tetrahydroborate体系中,用 四氢呋喃 作为反应溶剂,化学反应 1.0H,以85%的收率获得产物2-噻吩磺酰胺 参考文献:Obafemi,Craig. A.; Onigbinde,Adebayo O.,Phosphorus,Sulfur And Silicon And The Related Elements,1991,Vol. 57,# 1/2,P. 75-81 标题:Obafemi,Craig. A.; Onigbinde,Adebayo O.,Phosphorus,Sulfur And Silicon And The Related Elements,1991,Vol. 57,# 1/2,P. 75-81
专利信息
专利号:EP-2054420-B1 优先权日:2006-08-02 标题:Benzimidazo[1,2-c][1,2,3]thiadiazol-7-sulfonamides as inhibitors of carbonic anhydrase and the intermediates for production thereof 发明人:MATULIS DAUMANTAS; DUDUTIENE VIRGINIJA; MATULIENE JURGITA; MISTINAITE LINA 权利人:BIOTECHNOLOGIJOS INST 摘要:The invention is related to novel compounds - benzimidazo[1,2-c][1,2,3]thiadiazole sulfonamides, corresponding to the general formula (I). The compounds can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit enzymes which participate in disease progression such as glaucome. The compounds of formula (I) inhibits enzymes such as carbonic anhydrases and metallo proteinases. This invention is also related to new intermediate compounds which are used for the synthesis of sulfonamides of formula (I).
专利号:US-6800764-B2 优先权日:2001-12-11 标题:Process for the synthesis of chirally pure beta-amino-alcohols 发明人:KREFT ANTHONY FRANK; ANTANE MADELENE MIYOKO; COLE DEREK CECIL; KUBRAK DENNIS MARTIN; RESNICK LYNN; STOCK JOSEPH RAYMOND; WANG ZHENG 权利人:WYETH CORP 摘要:A process is provided for preparing chirally pure S-enantiomers of alpha-amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the formula (R)2CH(CH2)nCH2X; b) adding the organometallic reagent to carbon dioxide to afford a carboxylic acid; c) activating the carboxylic acid with an acid chloride, phosphorus trichloride, acid anhydride, or thionyl chloride in the presence of a tertiary amine base; d) reacting the product of step c) with an alkali metal salt of S-4-benzyl-2-oxazolidinone; e) treating the product of step d) with a strong non-nucleophilic base to form an enolate anion; f) trapping the enolate anion with 2,4,6-triisopropylbenzenesulfonyl azide to afford an oxazolidinone azide; g) hydrolyzing the oxazolidinone azide with an aqueous base to afford an alpha-azido acid; h) reducing the alpha-azido acid to the alpha-amino acid; and i) recrystallizing the alpha-amino acid to the chirally pure alpha-amino acid. A process is also provided for preparing chirally pure S-enantiomers of beta-amino alcohols further comprising the steps of reducing the crude alpha-amino acid to the beta-amino alcohol and recrystallizing the beta-amino alcohol to the chirally pure beta-amino alcohol. A process is further provided for preparing chirally pure S enantiomers of N-sulfonyl beta-amino alcohols further comprising the steps of sulfonylating the beta-amino alcohol with 5-chloro-thiophene-2-sulfonyl halide; and recrystallizing to afford the chirally pure N-sulfonyl beta-amino alcohols.
专利号:US-7074921-B2 优先权日:2001-11-13 标题 :Process for the preparation of 3,7-disubstituted-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine compounds 发明人:KRONENTHAL DAVID R; BHANDARU RAO S; SHI ZHONGPING; MUDRYK BOGUSLAW M 权利人:BRISTOL MYERS SQUIBB CO 摘要:Methods for the synthesis of benzodiazepine compounds having farnesyl protein transferase inhibitory activity.
专利号:US-2003144531-A1 优先权日:2001-12-11 标题 :Process for the synthesis of chirally pure beta-amino-alcohols
专利号:CN-1602290-A 优先权日:2001-12-11 标题 :Process for the synthesis of chirally pure beta -amino-alcohols
专利号:US-8344136-B2 优先权日:2008-06-16 标题:Process for the preparation of brinzolamide 发明人:FALCHI ALESSANDRO; DE LUCCHI OTTORINO; CASTELLIN ANDREA 权利人:PHF S A; FALCHI ALESSANDRO; DE LUCCHI OTTORINO; CASTELLIN ANDREA 摘要:The present invention relates to a process for the preparation of Brinzolamide, or 2H-thieno[3,2-e]-1,2-thiazin-6-sulfonamide, 4-(ethyl amino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (4R)-via intermediates 2,3-dihydro-4H-thieno[3,2-e]-1,2-thiazin-4-ones, 1,1-dioxide. Further objects of the present invention are the intermediates mentioned above and other intermediates of the synthesis.