CAS: 541-16-2; 1,3-Bis(1,1-Dimethylethyl) Propanedioate

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CAS号141-82-2 丙二酸 | CAS号75-65-0 叔丁醇 | CAS号1663-67-8 丙二酰氯 | CAS号115-11-7 2-甲基丙烯 | CAS号1204142-47-1 2-(hydroxy-phen... | CAS号504-64-3 二氧化三碳 | CAS号4326-36-7 B°C-L-酪氨酸甲酯 | CAS号23550-28-9 2-[((叔丁基)氧基羰基]丁... | CAS号79099-07-3 1-B°C-4-哌啶酮 | CAS号621-84-1 氨基甲酸苄酯 | CAS号87376-41-8 1,1-di-tert-but... | CAS号87376-40-7 1,1,3,3-tetra-t... | CAS号35207-75-1 Propanedioicaci... | CAS号34812-95-8 1,3-Di-tert-but... | CAS号35207-83-1 Bicyclo[4.1.0]h... | CAS号157634-00-9 N-B°C-2-哌啶甲醇

Di-Tert-Butyl 2-Bromomalonate置于(Brbu2Te)2O 亚磷酸三苯酯,碳酸氢钠体系中,用 水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 5.0H,以81%的收率获得产物丙二酸二叔丁酯
参考文献:Wittig型和脱卤反应的意外催化剂.
标题:Wittig型和脱卤反应的意外催化剂.
摘要:开发了用于维蒂希型和脱卤反应的新型催化剂2.在亚磷酸三苯酯的存在下,当使用1-2 Mol%的化合物2时,各种各样的醛可以与α-溴乙酸酯反应,以高收率提供具有出色的e-立体选择性的α,β-不饱和酯或酮.化合物2还是用于α-溴羰基化合物的还原脱卤的有效催化剂.还提出了上述反应的机理.
DOI:10.1021/jo025693B

专利信息

专利号:US-2004266827-A1
优先权日:2003-06-25
标 题 :Convergent asymmetric route to produce a key intermediate towards the synthesis of a garft inhibitor
发明人：NOTZ WOLFGANG REINHARD LUDWIG; MARTINEZ CARLOS ALBERTO
权利人:AGOURON PHARMA
摘要:The invention relates to processes for the preparation of a key intermediate in the synthesis of a GARFT inhibitor of formula (Ia) containing a 4-methyl-substituted thiophene core: n n n wherein said key intermediate has the following formula (I): n n n wherein each of R 1 and R 2 are independently a moiety that together with the attached CO 2 forms a readily hydrolyzable ester group; n from a compound of the formula (VI): n n n wherein R 1 is as described above, Pg 1 is an amino protecting group, and Pg 2 is an ether protecting group; wherein said processes are as described in the specification.

专利号:US-6818777-B2
优先权日:2000-12-07
标 题:Intermediates for synthesis of vinblastine compound and method for synthesizing the intermediate
发明人：FUKUYAMA TOHRU; TOKUYAMA HIDETOSHI
权利人:JAPAN SCIENCE & TECH AGENCY
摘要:Intermediates A, which are important in the whole synthesis of vindoline; and a method of synthesizing intermediates respectively represented by the general formulae B and C. By the method, the target intermediates are effectively synthesized with satisfactory reproducibility. This synthesis method is especially suitable for mass production. General formula A General formula B General formula C.

专利号:US-4283536-A
优先权日:1977-12-29
标 题:Preparation of vincadifformine and related derivatives
发明人：KUEHNE MARTIN E
权利人:UNIV VERMONT
摘要:This invention relates to the preparation of vincadifformine and related derivatives which are useful as starting material for the synthesis of among other alkaloids vincamine and other similar compounds possessing interesting psychopharmacologic properties. n A tetrahydro-β-carboline (II) is reacted with benzoyl chloride to provide a 2-benzoyl-1,2,3,4-tetrahydro-9H-pyrido-(3,4-b)-indole (III). Then compound (III) is reduced to give a 2-benzyl-1,2,3,4-tetrahydro-9H-pyrido-(3,4-b)-indole (IV). Thereafter, compound (IV) is transformed by t-butyl hypochlorite into a chloroindolenine derivative (V) which is immediately treated with a metal dialkylmalonate such as thallium t-butyl methyl malonate to give a dialkyl 3-benzyl-1,2,3,4,5,6-hexahydroazepino-(4,5-b)-indole-5,5-dicarboxylate (VI). Compound (VI) is then partly decarboxylated into a alkyl 3-benzyl-1,2,3,4,5,6-hexahydro-(4,5-b) indole-5-carboxylate (VII). Compound (VII) is hydrogenated to give an alkyl 1,2,3,4,5,6-hexahydroazepino-(4,5-b)-indole 5-carboxylate (VIII). In an alternative embodiment, compound (VI) can be hydrogenated to the corresponding dialkyl 1,2,3,4,5,6-hexahydroazepino-(4,5-b)-indole-5,5-dicarboxylate which is then decarboxylated into compound (VIII). Compound (VIII) is condensed with a functionalised aldehyde, typically a epoxy aldehyde or a haloaldehyde such as 1-bromo-4-formylhexane, to give vincadifformine or similar pentacyclic derivatives.

专利号:US-5280126-A
优先权日:1988-02-22
标题 :Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
发明人：BUTLER DONALD E; DEERING CARL F; MILLAR ALAN; NANNINGA THOMAS N; ROTH BRUCE D
权利人:WARNER LAMBERT CO
摘要:An improved process for the preparation of trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where 1,6-heptadien-4-ol is converted in eight operations to the desired products, as well as an improved process for the preparation of (2R-trans) and trans-(±)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide by a novel synthesis where 4-methyl-3-oxo-N-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-α-[2-methyl-1-oxopropyl]-Y-oxo-N,β-diphenylbenzenebutaneamide is converted in one step to the desired product, and additionally, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide from (R)-4-cyano-3-[[(1,1-dimethylethyl)dimethylsilyl]oxy]butanoic acid, as well as other valuable intermediates used in the processes.

专利号:US-5216174-A
优先权日:1988-02-22
标题:Process for trans-6-[12-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
发明人：BUTLER DONALD E; DEERING CARL F; MILLAR ALAN; NANNINGA THOMAS N; ROTH BRUCE D
权利人:WARNER LAMBERT CO
摘要:An improved process for the preparation of trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where 1,6-heptadien4-ol is converted in eight operations to the desired products, as well as an improved process for the preparation of (2R-trans) and trans-(±)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3carboxamide by a novel synthesis where 4-methyl-3-oxoN-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-α-[2methyl-1-oxopropyl]-γ-oxo-N,β-diphenylbenzenebutaneamide is converted in one step to the desired product, and additionally, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1Hpyrrole-3-carboxamide from (R)-4-cyano-3-[[(1,1-dimethylethyl)dimethylsilyl]oxy]butanoic acid, as well as other valuable intermediates used in the processes.

专利号:US-5097045-A
优先权日:1989-02-01
标题 :Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
发明人：BUTLER DONALD E; DEERING CARL F; MILLAR ALAN; NANNINGA THOMAS N; ROTH BRUCE D
权利人:WARNER LAMBERT CO
摘要:An improved process for the preparation of trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where 1,6-heptadien-4-ol is converted in eight operations to the desired products, as well as an improved process for the preparation of (2R-trans) and trans-(±)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]1H-pyrrole-3-carboxamide by a novel synthesis where 4-methyl-3-oxo-N-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-α-[2-methyl-1-oxopropyl]-γ-oxo-N,β-diphenylbenzenebutaneamide is converted in one step to the desired product, and additionally, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide from (R)-4-cyano-3-[[(1,1-dimethylethyl)dimethylsilyl]oxy]butanoic acid, as well as other valuable intermediates used in the processes.