CAS: 13388-75-5; 2-(3,5-Dimethoxyphenyl)Acetonitrile

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3,5-二甲氧基苯甲醛置于硼烷四氢呋喃络合物,甲基磺酰氯,三乙胺体系中,用 四氢呋喃,N-甲基吡咯烷酮 用作溶剂,化学反应 17.0H,反应生成3,5-二甲氧基苯基乙腈
参考文献:糖肽类抗生素的突变合成:万古霉素 Ab 环氨基酸 3,5-二羟基苯基甘氨酸的变异
标题:糖肽类抗生素的突变合成:万古霉素 Ab 环氨基酸 3,5-二羟基苯基甘氨酸的变异
摘要:在突变合成方法中,万古霉素型糖肽抗生素生产者 Amycolatopsis Balhimycina 的 Deltadpga 突变体在 3,5-二羟基苯基甘氨酸 (Dpg) 的合成中存在缺陷,补充了合成的 Dpg 类似物以获得相应的修饰糖肽.空间上要求更高的 3,5-二取代甲氧基衍生物以及单取代 Dpg 类似物被接受为底物.这些事实表明,空间和电子要求在几种情况下足以使 Ab 环氧化闭合,从而导致产生新的抗生素活性糖肽衍生物.结果代表了评估肽次生代谢物突变合成潜力的进一步步骤.
Doi:10.1021/ja0499389

专利信息

专利号:US-4072716-A
优先权日:1971-12-24
标 题:Bicycloalkane derivatives
发明人：SAUER GERHARD; HAUSER HELMUT; HAFFER GREGOR; RUPPERT JUERGEN; EDER ULRICH; WIECHERT RUDOLF
权利人:SCHERING AG
摘要:Bicycloalkane derivatives of the formula ##STR1## WHEREIN N IS 1 OR 2, R 1 is lower alkyl, X is carbonyl or free or etherified hydroxymethylene, and Y is --S--R 2 , --SO m --R 2 , or ##STR2## wherein m is 1 or 2, R 2 is alkyl, R 3 is hydrogen or lower alkyl, R 4 is aliphatic acyl and Z is nitro, lower alkanoyl, lower alkylsulfinyl, or lower alkylsulfonyl are useful intermediates in the total synthesis of steroids. The compounds are prepared by reacting a corresponding compound lacking the CH 2 Y substituent with formaldehyde and a mercaptan or a sulfinic acid, followed if desired by oxidation and optional salt condensation.

专利号:US-4051188-A
优先权日:1971-12-24
标题 :Novel bicycloalkane derivatives and the production thereof
发明人：SAUER GERHARD; HAUSER HELMUT; HAFFER GREGOR; RUPPERT JUERGEN; EDER ULRICH; WIECHERT RUDOLF
权利人:SCHERING AG
摘要:Bicycloalkane derivatives of the formula ##STR1## WHEREIN N IS 1 OR 2, R 1 is lower alkyl, X is carbonyl or a free or etherified hydroxymethylene, and Y is --S--R 2 , --SO m --R 2 , or ##STR2## wherein m is 1 or 2, R 2 is aryl or aralkyl, R 3 is hydrogen or lower alkyl, R 4 is phenyl optionally substituted with lower alkoxy or benzyloxy, and Z is nitro, lower alkanoyl, lower alkylsulfinyl, or lower alkylsulfonyl, are useful intermediates in the total synthesis of steroids. The compounds are prepared by reacting a corresponding compound lacking the CH 2 Y substituent with formaldehyde and a mercaptan or a sulfinic acid, followed if desired by oxidation and optional salt condensation.

专利号:US-4008253-A
优先权日:1971-12-24
标题 :Bicycloalkanes
发明人：SAUER GERHARD; HAUSER HELMUT; HAFFER GREGOR; RUPPERT JURGEN; EDER ULRICH; WIECHERT RUDOLF
权利人:SCHERING AG
摘要:Bicycloalkane derivatives of the formula ##STR1## WHEREIN N IS 1 OR 2, R 1 is lower alkyl, X is free or ketalized carbonyl or a free, esterified, or etherified hydroxymethylene, and Y is --S--R 2 , --SO m --R 2 , or ##STR2## wherein m is 1 or 2, R 2 is alkyl, aryl, or aralkyl, R 3 is hydrogen or lower alkyl, R 4 is alkoxycarbonyl, or acyl or phenyl optionally substituted with lower alkoxy or benzyloxy- or acyloxy; and Z is nitrile, nitro, lower alkoxycarbonyl, lower alkanoyl, lower alkylsulfinyl, or lower alkylsulfonyl are useful intermediates in the total synthesis of steroids. The compounds are prepared by reacting a corresponding compound lacking the CH 2 Y substituent with formaldehyde and a mercaptan or a sulfinic acid, followed if desired by oxidation and optional salt condensation.

专利号:US-4202991-A
优先权日:1971-12-24
标 题:Novel bicycloalkane derivatives and the production thereof
发明人：EDER ULRICH; HAFFER GREGOR; HAUSER HELMUT; RUPPERT JUERGEN; SAUER GERHARD; WIECHERT RUDOLF
权利人:SCHERING AG
摘要:Bicycloalkane derivatives of the formula ##STR1## wherein n is 1 or 2, R 1 is lower alkyl, Acyl is alkanoyl, and Y is --S--R 2 , --SO m --R 2 , or ##STR2## wherein m is 1 or 2, R 2 is alkyl, R 3 is hydrogen or lower alkyl, R 4 is acyl or phenyl optionally substituted with lower alkoxy, benzyloxy or alkanoyloxy; and Z is nitro, lower alkoxycarbonyl, lower alkanoyl, lower alkylsulfinyl, or lower alkylsulfonyl are useful intermediates in the total synthesis of steroids. The compounds are prepared by reacting a corresponding compound lacking the CH 2 Y substituent with formaldehyde and a mercaptan or sulfinic acid, followed if desired by oxidation and optional salt condensation.

专利号:US-9884842-B2
优先权日:2013-04-19
标题 :Combretastatin analogs
发明人：PENTHALA NARSIMHA REDDY; CROOKS PETER; SONAR VIJAYAKUMAR
权利人:UNIV ARKANSAS; BIOVENTURES LLC
摘要:The present invention relates novel heterocyclic analogs of combretastatin, their synthesis, and their use as anti-cancer compounds. In particular, compounds of Formula (I), Formula (II), and Formula (V) are provided.

专利号:WO-2024159288-A1
优先权日:2023-01-30
标 题:Nav1.7- and/or nav1.8-inhibiting amides, processes for the preparation thereof, compositions, uses, methods for treatment using same, and kits
发明人：BARREIRO GABRIELA; SANT'ANA DANILO PEREIRA DE; MONTEIRO JÚLIA LAMMOGLIA; GAMBA LUIS EDUARDO REINA; LIMA LÃ?DIA MOREIRA; FRAGA CARLOS ALBERTO MANSSOUR; BARREIRO ELIEZER JESUS DE LACERDA
权利人:EUROFARMA LABORATORIOS S A; UNIV FEDERAL DO RIO DE JANEIRO – UFRJ
摘要:The present invention relates to Nav1.7- and/or Nav1.8-inhibiting amides. More specifically, the present invention relates to amides comprising formula (I): (Ia) (Ib), in which the substituents R1 to R27 are selected independently of the groups defined in the description, as well as to processes for the preparation thereof, compositions comprising at least one of said compounds, uses, treatment methods for treating or preventing pain-related pathologies, and kits. The present invention pertains to the fields of medicinal chemistry and organic synthesis, as well as to the treatment of pain-related disorders.