CAS: 3144-16-9; ((1S,4R)-7,7-Dimethyl-2-Oxobicyclo[2.2.1]Heptan-1-yl)Methanesulfonic Acid

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CAS号464-49-3 D(+)-樟脑 | CAS号5872-08-2 混旋樟脑磺酸 | CAS号76-22-2 (±)-樟脑(合成) | CAS号76-26-6 [7,7-dimethyl-2... | CAS号7647-01-0 盐酸 | CAS号2935-35-5 (|S|)-(+)-α-苯甘氨酸 | CAS号357-57-3 马钱子碱 | CAS号108-24-7 乙酸酐 | CAS号1088994-09-5 ((3R,6R)-6-甲基哌啶... | CAS号21229-95-8 4-(benzenesulfi... | CAS号184850-95-1 (4S)-7,7-dimeth... | CAS号94594-90-8 左旋樟脑磺内酰胺 | CAS号6515-36-2 7-羟基黄烷酮 | CAS号60886-80-8 (-)-10-樟脑内磺酰亚胺 | CAS号71242-58-5 (1S)-(-)-10-巯基异冰片 | CAS号56-75-7 氯霉素 | CAS号134-90-7 L-(+)-氯霉素 | CAS号60933-63-3 (1S)-10-樟脑内磺酰胺

(1S)-10-Camphorsulfonamide置于pyrilium Tetrafluoroborate,Magnesium Chloride体系中,用 叔丁醇 作为反应溶剂,化学反应 5.0H,以86%的收率获得产物d(+)-10-樟脑磺酸
参考文献:由pyry-Bf4活化的磺酰胺选择性地形成后期磺酰氯.
标题:由pyry-Bf4活化的磺酰胺选择性地形成后期磺酰氯.
摘要:此处报道的是通过吡喃鎓盐(pyry-Bf4)与亲核试剂一起对伯磺酰胺进行简单实用的官能化.这种简单的试剂可以活化磺酰胺中不良的亲核nh 2基团,从而可以形成有机合成中最好的亲电试剂之一:磺酰氯.由于在药物环境中伯磺酰胺的多样性,因此特别注意集中在通过后期形成相应的磺酰氯而直接转化为稠密官能化的伯磺酰胺.多种亲核试剂可参与该转化,因此允许合成复杂的磺酰胺,磺酸盐,硫化物,磺酰氟和磺酸.
DOI:10.1002/anie.201910895

专利信息

专利号:US-8138330-B2
优先权日:2006-09-11
标 题 :Process for the synthesis of oligonucleotides
发明人：LEUCK MICHAEL; WOLTER ANDREAS; STUMPE ALFRED
权利人:LEUCK MICHAEL; WOLTER ANDREAS; STUMPE ALFRED; SIGMA ALDRICH CO LLC
摘要:The present invention discloses novel methods for the synthesis of oligonucleotides with nucleoside phosphoramidites on solid supports. The methods comprise the stepwise chain assembly of oligonucleotides on supports with 5′-acyl phosphoramidites. The synthesis cycles consist of a front end deprotection step which is conducted with a solution of a primary amine or a phenolate, a phosphoramidite coupling step with a 5′-acyl nucleoside phosphoramidite in the presence of an activator, a phosphite oxidation step and an optional capping step. The novel methods improve the quality of synthetic oligonucleotides due to the irreversibility of the front end deprotection step, which prevents the formation of deletion sequences, and due to the avoidance of acidic reagents in the synthesis cycles, which prevent the formation of depurination side products. The invention further discloses novel nucleoside phosphoramidite compositions wherein the phosphoramidites carry acyl front end protective groups which are cleavable with primary amines or phenolates. The invention is applicable to the synthesis of oligodeoxyribonucleotides, oligoribonucleotides and oligonucleotides with modifications in their sugar or phosphate groups.

专利号:US-2008032964-A1
优先权日:2006-04-10
标题:Process for the synthesis of azetidinone
发明人：KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO
权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO
摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.

专利号:US-2004018598-A1
优先权日:2000-05-30
标题 :Bio-intermediates for use in the chemical synthesis of polyketides
发明人：SANTI DANIEL; ASHLEY GARY; MYLES DAVID C
摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.

专利号:US-2012165520-A1
优先权日:2010-12-23
标题:Process for the synthesis of prodrugs of opioids
发明人：MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS
权利人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS
摘要:The present invention provides a process for the synthesis of opioid prodrugs. In particular, the present invention provides a process for the synthesis of opioid prodrugs comprising: treating an opioid, in the form of a salt or a freebase, with a carbonyl synthon to form an activated intermediate and subsequently reacting the activated intermediate with an amine, in the form of a salt or a freebase.

专利号:WO-2010078250-A1
优先权日:2008-12-30
标 题:Synthesis of (2-amino)-tetrahydrocarbazole-propanoic acid
发明人：WEI YUAN; Li tianqiao; CHI YONGXIANG; ZHU JINGYANG
权利人:CHIRAL QUEST INC; WEI YUAN; Li tianqiao; CHI YONGXIANG; ZHU JINGYANG
摘要:The present invention provides a new approach to the synthesis of 2-amino-tetrahydrocarbazole-propanoic acid, a key intermediate for the synthesis of Ramatroban. More specifically, a synthesis of 2-amino-tetrahydrocarbazole- propanoic acid which includes oxidizing an aminocyclohexanol to form an aminocyclohexanone, condensing the aminocyclohexanone to form a tetrahydrocarbazole, deprotecting the tetrahydrocarbazole to yield a racemic mixture of a tetrahydrocarbazole, resolving the racemic mixture to obtain a yield mixture with an enantiomeric excess of one enantiomer over another, alkylating the excess enantiomer to yield an alkyl ester, and hydrolyzing the alkyl ester to yield 2-amino-tetrahydrocarbazole-propanoic acid.

专利号:US-4910310-A
优先权日:1988-10-03
标 题:Synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives
发明人：CAMPBELL ARTHUR L; BEHLING JAMES R; BABIAK KEVIN A; NG JOHN S; MUELLER RICHARD A; FLEET GEORGE W J
权利人:SEARLE & CO
摘要:Novel intermediates and method for the chemical synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives are provided. A preferred intermediate is 1,5-dideoxy-1,5-imino-3, 4-O-isopropylidene-L-fucitol which is used to prepare the HIV inhibitor 1,5-dideoxy-1,5-imino-[N-ω-methyl caproate]-L-fucitol. These compounds are prepared in a short synthesis from the known compound 2,3-O-isopropylidene-D-lyxono-1,4-lactone or in a multi-step synthesis from D-galactose.