CAS: 39687-95-1; Methyl Isocyanoacetate

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5680-79-5 7148-06-3 616-34-2

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N-甲酰甘氨酸甲酯置于三乙胺,三氯氧磷体系中,用 二氯甲烷 用作溶剂,化学反应生成异腈基乙酸甲酯
参考文献:炔砜在溶液中和在固体支持物上的1,3-偶极环加成反应.
标题:炔砜在溶液中和在固体支持物上的1,3-偶极环加成反应.
摘要:几种代表性的炔砜通过酯连接基固定在衍生自merrifield树脂的聚合物载体上,该酯连接基用于将固相载体上的游离羧酸基团与乙炔基的芳基磺酰基部分上的苄基羟基官能团偶联.还成功地制备了直接使用merrifield树脂制备的反向酯连接基的几个实例.用一系列1,3-偶极子研究了固体负载的乙炔砜的1,3-偶极环加成反应,包括叠氮化苄,重氮乙酸乙酯,重氮甲烷以及代表性的腈氧化物,腈亚胺,腈,亚硝酮,偶氮甲亚胺,偶氮甲亚胺,孟克农和sydnones.通常,在溶液相中也用炔砜进行类似的环加成反应以进行比较.环加成物通常在溶液相和固相中都提供所需产物的非常好至极好的收率,尽管后者反应有时需要更剧烈的条件.除了获得叠氮异构体混合物的苄基叠氮化物和重氮化合物外,其他1,3-偶极以高区域选择性反应并提供基本独特的区域异构体.通过碱水解顺利地从树脂上裂解产物,而除了从聚合物上裂解之外,几次尝试用钠汞齐或二碘化sa-
Doi:10.1021/jo801621D

专利信息

专利号:US-6376649-B1
优先权日:1998-12-18
标题 :Methods for the synthesis of α- hydroxy-β-amino acid and amide derivatives
发明人：SEMPLE JOSEPH E; LEVY ODILE E
权利人:CORVAS INT INC
摘要:Methods for the synthesis of alpha-hydroxy-beta-amino acid and amide derivatives and alpha-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehyde with an isonitrile and a carboxylic acid to give an amino-alpha-acyloxy carboxamide. The acyloxy group may be removed to give the derivative. Alternatively the protecting group is removed and acyl shift occurs to give the derivative. These derivatives are useful in the synthesis of compounds such as peptidyl alpha-ketoamides and alpha-hydroxy-beta-carboxylic acid and amide derivatives. Certain of these compounds have been reported to have activity as inhibitors of proteases, such as serine proteases and cysteine proteases.

专利号:US-2012203004-A1
优先权日:2009-08-13
标题 :process for the synthesis of alkyl/aralkyl (2s)-2-(tert-butoxycarbonyl)-amino-2-[-8-azabicyclo[3.2.1]oct-3-yl]-exo-acetate and analogs thereof: key intermediates for the preparation of dppiv inhibitors
发明人：ROY BHAIRAB NATH; KAMBOJ RAJENDER KUMAR; GOERGE SHAJI K; VENUGOPAL SPINVIN C; SHANMUGVADIVELU MUTHU KUMARAN; SINHA NEELIMA
权利人:ROY BHAIRAB NATH; KAMBOJ RAJENDER KUMAR; GOERGE SHAJI K; VENUGOPAL SPINVIN C; SHANMUGVADIVELU MUTHU KUMARAN; SINHA NEELIMA; LUPIN LTD
摘要:An improved process for the synthesis of intermediates like Alkyl/Aralkyl (2S)-2-(tert-butoxycarbonyl)-amino-2-[-8-azabicyclo[3.2.1]oct-3-yl]-exo-acetate and analogs thereof which are useful in the synthesis of Dipeptidyl peptidase-IV (DP-PIV) inhibitors.

专利号:US-2003083352-A1
优先权日:2000-07-31
标 题 :Synthesis of imidazole intermediates
发明人：HELAL CHRISTOPHER J
权利人:PFIZER
摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.

专利号:WO-9502566-A1
优先权日:1993-07-16
标题 :Synthesis of combinatorial arrays of organic compounds through the use of multiple component combinatorial array syntheses
发明人：ARMSTRONG ROBERT W
权利人:UNIV CALIFORNIA; ARMSTRONG ROBERT W
摘要:The present invention relates to an array of compounds having a common core structure wherein the compounds of the array comprise the products of a multiple component combinatorial array synthesis having at least three components. The present invention also relates to the method of synthesizing that array. A further embodiment of the present invention relates to the use of solid phase synthesis to synthesize the combinatorial array of compounds. The present invention also relates to a method of creating a combinatorial array of compounds with a common core structure by identifying the desired core structure, identifying an MCCA reaction capable of generating that core structure, followed by preparing an array of compounds using the identified MCCA reaction according to the aforementioned method. The present invention also relates to a method for conducting in vitro assays of biological material using the combinatorial arrays of the present invention.

专利号:US-8563763-B2
优先权日:2011-04-05
标 题 :Composition, synthesis and use of isonitriles
发明人：FLEMING FRASER FERGUSON; PITTA BHASKAR REDDY
权利人:FLEMING FRASER FERGUSON; PITTA BHASKAR REDDY; UNIV HOLY GHOST DUQUESNE
摘要:The present invention relates to isonitrile compounds, methods of synthesis, and uses in a variety of fields. In one aspect, the present invention includes sulfinyl methyl isonitriles and methods for their preparation. In another aspect, the present invention includes the use of sulfinyl methyl isonitriles to prepare various other isonitrile compounds and derivatives thereof. In yet another aspect, the present invention includes a relatively simple and routine synthesis of sulfinyl methyl isonitrile compounds, other isonitrile compounds and derivatives thereof.

专利号:US-8012993-B2
优先权日:2006-12-28
标题 :Stable S-nitrosothiols, method of synthesis and use
发明人：MOLINER JOSE REPOLLES; COY FRANCISCO PUBILL; MANCINI MARISABEL MOURELLE; NIETO JUAN CARLOS DEL CASTILLO; LLORENTE LYDIA CABEZA; BONIN JUAN MARTINEZ; SALADRIGAS ANA MODOLELL
权利人:LACER SA
摘要:The present invention relates to stable S-nitrosothiols derivatives of formula (I) n nhaving vasodilating effect and which inhibit the aggregation of the platelets and which therefore are useful for the preparation of medicaments for treatment of NO related diseases. The invention also relates to a process for the synthesis of the compounds of formula (I).