罂粟碱置于rat Liver Enzymes,Silver(I) Chloride体系中,用 乙腈 用作溶剂,化学反应 4.0H,反应生成3,4-二甲氧基苯甲醛 参考文献:Pseudobase Formation In 2-Methylpapaverinium Cations And Their Biotransformation By Enzymes Of Rat Liver Homogenates In Vitro 标题:Pseudobase Formation In 2-Methylpapaverinium Cations And Their Biotransformation By Enzymes Of Rat Liver Homogenates In Vitro 摘要:2-甲基罂粟碱碘化物(i),2'-羟甲基-2-甲基罂粟碱碘化物(ix),和2-甲基-3,4-二氢罂粟碱碘化物(x. Ch3I)通过将氢氧根离子加到c(1)=n(+)键形成伪碱基.2'-羟甲基-2-甲基-3,4-二氢罂粟碱碘化物(xv)和2'-羟甲基-2-甲基-9-氧代-3,4-二氢罂粟碱碘化物(xvi)在水性介质中与氢氧根离子反应,形成环状伪碱基xvii和xviii.在水性乙醇(1:1 W/w,25°C,离子强度0.1)中测定了伪碱基形成的平衡常数(kr+).季铵罂粟碱衍生物通过大鼠肝酶代谢为异喹啉酮和羰基化合物.讨论了伪碱基在这些生物转化中的作用,并得出了生物合成的结论. Doi:10.1135/cccc19800956
专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-8779122-B2 优先权日:2012-11-08 标 题:Process for the synthesis of (2E)-3-(3,4-dimethoxyphenyl)prop-2-enenitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:CARRANZA MARIA DEL PILAR; GARCIA ARANDA MARIA ISABEL; GONZALEZ JOSÉ LORENZO; SANCHEZ FRÉDÉRIC 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
专利号:US-8779123-B2 优先权日:2012-12-06 标题:Process for the synthesis of 3-(2-bromo-4,5-dimethoxyphenyl)propanenitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:CARRANZA MARIA DEL PILAR; GARCIA ARANDA MARIA ISABEL; GONZALEZ JOSÉ LORENZO; SANCHEZ FRÉDÉRIC 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
专利号:US-8779121-B2 优先权日:2012-10-12 标题:Process for the synthesis of 3-(2-bromo-4,5-dimethoxyphenyl)propanenitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:CARRANZA MARIA DEL PILAR; GARCIA ARANDA MARIA ISABEL; GONZALEZ JOSÉ LORENZO; SANCHEZ FRÉDÉRIC 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
专利号:US-10633360-B2 优先权日:2014-12-23 标题 :Efficient process for the synthesis of alkoxy substituted benzaldehydes 发明人:MOHAPATRA Manoj Kumar; BENDAPUDI Ramamohanrao; MENACHERRY Paul Vincent; PAUL VINCENT 权利人:ANTHEA AROMATICS PRIVATE LTD 摘要:The present invention relates to the synthesis of alkoxy substituted benzaldehydes obtained from the corresponding alkoxy substituted benzenes. Alkoxy substituted benzaldehydes are products of broad commercial interest and are used as end products and intermediates in flavor and fragrance applications and pharmaceutical ingredients. For example, 3,4-methylendioxy-benzaldehyde (also known as heliotropin or piperonal) is used widely both as a end product and intermediate for the above mentioned applications. Other examples include 3,4-dimethoxybenzaldehyde, 3,4,5-trimethoxybenzaldehyde and 3,4-ethylenedioxybenzene which are intermediates in the synthesis of active pharmaceutical intermediates.
专利号:US-9242925-B2 优先权日:2011-08-29 标题:Versatile and stereospecific synthesis of γ,δ-unsaturated amino acids by Wittig reaction 发明人:JUGE SYLVAIN; BAYARDON JEROME; REMOND EMMANUELLE; ONDEL-EYMIN MARIE-JOELLE 权利人:JUGE SYLVAIN; BAYARDON JEROME; REMOND EMMANUELLE; ONDEL-EYMIN MARIE-JOELLE; CENTRE NAT RECH SCIENT; UNIV BOURGOGNE 摘要:The γ,δ-unsaturated α-amino acids of general formula (I). Also, a versatile process for the stereospecific synthesis of said compounds of formula (I), involving a Wittig reaction. Further, intermediate products of general formulae (II) and (III), as shown below, which are involved in the synthesis of compounds (I). n n n n n n n n n n n n Compounds of general formula (I) may be useful as therapeutic substances, or as reagents or intermediates for fine chemistry.
[参考文献]: Ashley A Reinke, Et Al. A Chemical Screening Approach Reveals That Indole Fluorescence Is Quenched By Pre-Fibrillar But Not Fibrillar Amyloid-Beta. Bioorg Med Chem Lett. 2009 Sep 1;19(17):4952-7. [参考文献]: Carol Larroy, Et Al. Characterization Of The Saccharomyces Cerevisiae Ymr318C (Adh6) Gene Product As A Broad Specificity Nadph-Dependent Alcohol Dehydrogenase: Relevance In Aldehyde Reduction. Biochem J. 2002 Jan 1;361(Pt 1):163-72. [参考文献]: Daniele Tedesco, Et Al. Stopped-Flow Enantioselective Hplc-Cd Analysis And Td-Dft Stereochemical Characterization Of Methyl Trans-3-(3,4-Dimethoxyphenyl)Glycidate. Chirality. 2015 Dec;27(12):914-8. [参考文献]: Jong H Kim, Et Al. Identification Of Phenolics For Control Of Aspergillus Flavus Using Saccharomyces Cerevisiae In A Model Target-Gene Bioassay. J Agric Food Chem. 2004 Dec 29;52(26):7814-21. [参考文献]: K Kónya, Et Al. Antioxidant Properties Of 8.0.4'-Neolignans. Phytomedicine. 2001 Nov;8(6):454-9.