Benzoyl meso-tartaric acid | 65621-34-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: Benzoyl meso-tartaric acid
• 英文别名: 2-benzoyloxy-3-hydroxybutanedioic acid
• CAS: 65621-34-3
• 化学式: C₁₁H₁₀O₇
• 分子量: 254.19
• InChiKey: JXXURQWKKCNUBH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  18
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  121
• 氢给体数：
  3
• 氢受体数：
  7

文献信息

• [EN] QUINOXALINONE DERIVATIVES AS INSULIN SECRETION STIMULATORS, METHODS FOR OBTAINING THEM AND USE THEREOF FOR THE TREATMENT OF DIABETES<br/>[FR] DÉRIVÉS DE QUINOXALINONE COMME STIMULATEURS DE LA SÉCRÉTION D'INSULINE, LEURS PROCÉDÉS D'OBTENTION ET LEUR UTILISATION POUR LE TRAITEMENT DU DIABÈTE
  申请人：MERCK PATENT GMBH

  公开号：WO2009109258A1

  公开（公告）日：2009-09-11

  The present invention relates to quinoxalinone derivatives of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these quinoxalinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated. Other preferred compounds are compounds of general formula (I), wherein R1, R2, R3, R4, R5 and R6 can be optionally substituted by one or more groups selected from Z.

  本发明涉及式(I)的喹喔啉酮衍生物，其中R1、R2、R3、R4、R5和R6如权利要求1所定义，作为胰岛素分泌刺激剂。该发明还涉及这些喹喔啉酮衍生物的制备和用途，用于糖尿病和相关病理的预防和/或治疗。其他优选化合物是一般式(I)的化合物，其中R1、R2、R3、R4、R5和R6可以选择性地被来自Z的一个或多个基团取代。
• [EN] PREPARATION OF A BENZOIC ACID DERIVATIVE AND ITS USE FOR THE PREPARATION OF SUVOREXANT<br/>[FR] PRÉPARATION D'UN DÉRIVÉ D'ACIDE BENZOÏQUE ET SON UTILISATION POUR LA PRÉPARATION DE SUVOREXANT
  申请人：SANDOZ AG

  公开号：WO2016020403A1

  公开（公告）日：2016-02-11

  The present invention relates to a process for the preparation of a compound of formula (1) wherein the process is based on the use of an organolithium reagent and wherein Ra, Rb, Rc and Rd are, independently of each other, selected from the group consisting of H, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl, heterocycloalkyl, halogen, carbonyl, alkoxy, hydroxyl, -NR6R7, -SR and -NO2, wherein R6 and R7 are, independently of each other, selected from the group consisting of H, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl and heterocycloalkyl, and wherein E is an electrophilic group. The present invention further relates as to a compound obtained or obtainable by said method and to a compound of formula (1) as such. Further, the present invention relates to use of the compound of formula (1) for the preparation of Suvorexant.

  本发明涉及一种制备式（1）化合物的方法，该方法基于使用有机锂试剂，其中Ra、Rb、Rc和Rd分别独立地选自H、烷基、芳基、环烷基、杂原子烷基、杂原子芳基、杂原子环烷基、卤素、羰基、烷氧基、羟基、-NR6R7、-SR和-NO2的组成群，其中R6和R7分别独立地选自H、烷基、芳基、环烷基、杂原子烷基、杂原子芳基和杂原子环烷基的组成群，E是亲电性基团。本发明还涉及通过所述方法获得或可获得的化合物，以及式（1）化合物本身。此外，本发明涉及使用式（1）化合物制备Suvorexant。
• [EN] BENZOFURAN AMIDES AND HETEROAROMATIC ANALOGUES THEREOF FOR USE IN THERAPY<br/>[FR] AMIDES DE BENZOFURANE ET LEURS ANALOGUES HÉTÉROAROMATIQUES DESTINÉS À ÊTRE UTILISÉS EN THÉRAPIE
  申请人：EUROPEAN MOLECULAR BIOLOGY LABORATORY

  公开号：WO2018229193A1

  公开（公告）日：2018-12-20

  The present invention relatesto a pharmaceutical composition comprising acompound of the formula Ias described belowor a tautomeror a pharmaceutically acceptable salt thereof; to the compound of the formula Ias described below or a tautomer or a phar- maceutically acceptable salt thereof for use as a medicament, especially for use in the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularization, and to certain novel compoundsof the formula Ias described below or a tautomer or a pharmaceuti- cally acceptable salt thereof. Formula (I) wherein X1 is CR1 or N; X2 is CR2 or N; X3 is CR3 or N; X4 is CR4 or N; with the proviso that at most two of X1, X2, X3 and X4 are N; L1, L2 are a bond or a bivalent radical such as C1-C6-alkylene or C3-C8-cycloalkylene; A is 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated carbocyclic ring which may carry one or more substituents R9; or L2-A forms a group C1-C6-alkylene-OR13, C1-C6-alkylene-SR14 or C1-C6-alkylene-NR15R16; and R1, R2, R3, R4, R5, R6, R9, R13, R14, R15 and R16 are as defined in the claims and the description.

  本发明涉及一种药物组合物，包括下述的化合物I的构造或其互变异构体或药用盐；以及用作药物的下述的化合物I的构造或其互变异构体或药用盐，特别用于治疗或预防从炎症性疾病、过度增殖性疾病或紊乱、缺氧相关病理和以过度血管生成为特征的疾病中选择的疾病或紊乱；以及下述的某些新型化合物I的构造或其互变异构体或药用盐。其中，化合物(I)中X1为CR1或N；X2为CR2或N；X3为CR3或N；X4为CR4或N；但X1、X2、X3和X4中最多有两个为N；L1、L2为键或类似C1-C6-烷基或C3-C8-环烷基的二价基团；A为3-、4-、5-、6-、7-或8-成员饱和、部分不饱和或最大不饱和的碳环，可能携带一个或多个取代基R9；或L2-A形成一个基团C1-C6-烷基-OR13、C1-C6-烷基-SR14或C1-C6-烷基-NR15R16；而R1、R2、R3、R4、R5、R6、R9、R13、R14、R15和R16如权利要求和说明中所定义。
• METHOD FOR THE PREPARATION OF (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1-6-NAPHTHYRIDINE-3-CARBOX-AMIDE BY RACEMATE SEPARATION BY MEANS OF DIASTEREOMERIC TARTARIC ACID ESTERS
  申请人：Bayer Aktiengesellschaft

  公开号：US20210163474A1

  公开（公告）日：2021-06-03

  The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and also to the preparation of the enantiomer (Ia) by racemate resolution using chiral substituted tartaric acid esters of the general formulae (IIIa) and (IIIb) where Ar represents a substituted or unsubstituted aromatic or heteroaromatic radical.

  本发明涉及一种用于制备（4S）-4-(4-氰基-2-甲氧基苯基)-5-乙氧基-2,8-二甲基-1,4-二氢-1,6-萘啶-3-羧酰胺（I）的新型改进工艺，以及使用手性取代酒石酸酯（IIIa）和（IIIb）的一般式来进行外消旋分离制备对映体（Ia），其中Ar代表取代或未取代的芳香或杂芳基。
• [EN] PYRIDOPYRAZINONES DERIVATIVES INSULIN SECRETION STIMULATORS, METHODS FOR OBTAINING THEM AND USE THEREOF FOR THE TREATMENT OF DIABETES<br/>[FR] DÉRIVÉS DE PYRIDOPYRAZINONE COMME STIMULATEURS DE LA SÉCRÉTION D'INSULINE, LEURS PROCÉDÉS D'OBTENTION ET LEUR UTILISATION POUR LE TRAITEMENT DU DIABÈTE
  申请人：MERCK PATENT GMBH

  公开号：WO2009109341A1

  公开（公告）日：2009-09-11

  The present invention relates to pyridopyrazinone derivatives of formula (I), wherein X, Y, Z1 W, A and R1 are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these pyridopyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.

  本发明涉及式(I)的吡啶吡嗪酮衍生物，其中X、Y、Z1、W、A和R1如权利要求1所定义，作为胰岛素分泌刺激剂。该发明还涉及制备和使用这些吡啶吡嗪酮衍生物用于糖尿病和相关病理预防和/或治疗。