5,6-二苯基-2-吗啉酮 | 19180-79-1

• 物质功能分类: 有机原料 - 杂环化合物
• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 中文名称: 5,6-二苯基-2-吗啉酮
• 英文名称: (5,6)-diphenyl-morpholin-2-one
• 英文别名: 5,6-Diphenylmorpholin-2-one
• CAS: 19180-79-1
• 化学式: C₁₆H₁₅NO₂
• 分子量: 253.301
• InChiKey: LTPOSIZJPSDSIL-UHFFFAOYSA-N

物化性质

• 沸点：
  444.0±45.0 °C(Predicted)
• 密度：
  1.159

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  38.3
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2934999090
• 危险性防范说明：
  P261,P280,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H332,H335

文献信息

• [EN] MDM2 DEGRADERS AND USES THEREOF<br/>[FR] AGENTS DE DÉGRADATION DE MDM2 ET LEURS UTILISATIONS
  申请人：KYMERA THERAPEUTICS INC

  公开号：WO2021188948A1

  公开（公告）日：2021-09-23

  The present invention relates to compounds and methods useful for the modulation of mouse double minute 2 homolog ("MDM2") protein via ubiquitination and/or degradation by compounds according to the present invention.

  本发明涉及化合物和方法，通过本发明的化合物对小鼠双分子2同源蛋白（"MDM2"）蛋白进行泛素化和/或降解的调节。
• METHOD FOR SYNTHESIZING OPTICALLY ACTIVE a-AMINO ACID USING CHIRAL METAL COMPLEX COMPRISING AXIALLY CHIRAL N-(2-ACYLARYL)-2-[5,7-DIHYDRO-6H-DIBENZO[c,e]AZEPIN-6-YL] ACETAMIDE COMPOUND AND AMINO ACID
  申请人：HAMARI CHEMICALS, LTD.

  公开号：US20160102045A1

  公开（公告）日：2016-04-14

  Objects of the present invention are to provide an industrially applicable method for producing an optically active α-amino acid in high yield and in a highly enantioselective manner, to provide a simple production method of an optically active α,α-disubstituted α-amino acid, and to provide an intermediate useful for the above production methods of an optically active α-amino acid and an optically active α,α-disubstituted α-amino acid. The present invention provides a production method of an optically active α-amino acid or a salt thereof, the production method comprising introducing a substituent into the α carbon in the α-amino acid moiety of a metal complex represented by the following Formula (1): by an alkylation reaction, an aldol reaction, the Michael reaction, or the Mannich reaction, and releasing an optically pure α-amino acid enantiomer or a salt thereof by acid decomposition of the metal complex.

  本发明的目的是提供一种在高产率和高对映选择性的方式下生产光学活性α-氨基酸的工业上适用的方法，提供一种简单的生产方法，用于光学活性α，α-二取代的α-氨基酸，并提供一种用于上述光学活性α-氨基酸和光学活性α，α-二取代的α-氨基酸生产方法的中间体。本发明提供了一种光学活性α-氨基酸或其盐的生产方法，该生产方法包括通过烷基化反应、醛醇反应、迈克尔反应或曼尼希反应将取代基引入以下式（1）所表示的金属配合物的α-氨基酸基团的α碳中，并通过酸分解金属配合物释放光学纯α-氨基酸对映体或其盐。
• Phosphono/biaryl substituted dipeptide derivatives
  申请人：CIBA-GEIGY AG

  公开号：EP0511940A2

  公开（公告）日：1992-11-04

  Novel N-phosphonomethyl-biaryl substituted dipeptide derivatives of formula I wherein R and R' represent independently hydrogen, carbocyclic aryl, 6-tetrahydronaphthyl, 5-indanyl, acyloxymethyl or acyloxymethyl monosubstituted on methyl carbon by C1-C2o-alkyl, by C5-C7-cycloalkyl, by aryl or by aryl-lower alkyl ; A represents a direct bond, lower alkylene, phenylene or cyclohexylene ; m represents 1 or zero, provided that m represents 1 when A is a direct bond ; R1 represents phenyl, phenyl substituted by one to three substituents selected from lower alkyl, hydroxy, lower alkoxy, lower alkanoyloxy, halogen, cyano, trifluoromethyl, lower alkanoylamino or lower alkoxycarbonyl, naphthyl, naphthyl substituted by lower alkyl, lower alkoxy or halogen, thienyl, thienyl substituted by lower alkyl, furanyl, furanyl substituted by lower alkyl, pyridyl, pyridyl substituted by lower alkyl, halogen or cyano, pyrrolyl or N-lower alkylpyrrolyl ; R2 represents hydrogen, hydroxy, lower alkyl, aryl-lower alkyl, C5-C7-cycloalkyl-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, lower alkylthio-lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkylthio-lower alkyl or aryl-lower alkoxy-lower alkyl ; COR3 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester or amide ; and pharmaceutically acceptable salts thereof are useful as neutral endopeptidase (NEP) inhibitors. Suitable methods for their be manufacture are described.

  式 I 的新颖 N-膦酰甲基-叔丁基取代二肽衍生物 其中 R 和 R'独立地代表氢、碳环芳基、6-四氢萘基、5-茚基、酰氧基甲基或在甲基碳上被 C1-C2o- 烷基、C5-C7-环烷基、芳基或芳基-低级烷基单取代的酰氧基甲基；A 代表直接键、低级亚烷基、亚苯基或环己基；m 代表 1 或 0，但当 A 为直接键时，m 代表 1；R1 代表苯基、被选自低级烷基、羟基、低级烷氧基、低级烷酰氧基、卤素、氰基、 三氟甲基、低级烷酰胺基或低级烷氧基羰基的一至三个取代基取代的苯基、萘基被低级烷基、低级烷氧基或卤素取代的萘基，噻吩基，被低级烷基取代的噻吩基，呋喃基，被低级烷基取代的呋喃基，吡啶基，被低级烷基、卤素或氰基取代的吡啶基，吡咯基或 N-低级烷基吡咯基；R2代表氢、羟基、低级烷基、芳基-低级烷基、C5-C7-环烷基-低级烷基、氨基-低级烷基、羟基-低级烷基、低级烷硫基-低级烷基、低级烷氧基-低级烷基、芳基-低级烷硫基-低级烷基或芳基-低级烷氧基-低级烷基；COR3代表羧基或以药学上可接受的酯或酰胺形式衍生的羧基；其药学上可接受的盐可用作中性内肽酶（NEP）抑制剂。本文介绍了制造它们的适当方法。
• Biaryl substituted 4-amino-butyric acid amides
  申请人：CIBA-GEIGY AG

  公开号：EP0555175A1

  公开（公告）日：1993-08-11

  The invention relates to biaryl substituted 4-amino-butyric acid derivatives of formula I wherein COX and COX' independently represent carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester or amide; R1 represents hydrogen, lower alkyl, C3-C7-cycloalkyl-lower alkyl, aryl-lower alkyl, biaryl-lower alkyl, lower alkoxy, aryl-lower alkoxy, aryloxy, N-lower alkylamino, N,N-di-lower alkylamino, N-aryl-lower alkylamino, N,N-di-aryl-lower alkylamino, N-arylamino, N,N-diarylamino, lower alkanoylamino, aryl-lower alkanoylamino or aroylamino; R2 represents hydrogen, hydroxy, lower alkoxy, lower alkyl, aryl-lower alkyl, C3-C7-cycloalkyl-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, lower alkylthio-lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkylthio-lower alkyl or aryl-lower alkoxy-lower alkyl ; biaryl represents phenyl substituted by carbocyclic or heterocyclic aryl ; A represents a direct bond, lower alkylene, phenylene or cyclohexylene ; m represents 1 or zero, provided that m represents 1 when A is a direct bond ; or pharmaceutically acceptable salts thereof ; pharmaceutical compositions comprising said compounds ; methods for the preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of neutral endopeptidases by administration of said compounds to mammals in need of such treatment.

  本发明涉及式 I 的双芳基取代的 4-氨基丁酸衍生物 其中 COX 和 COX'独立地代表羧基或以药学上可接受的酯或酰胺形式衍生的羧基；R1 代表氢、低级烷基、C3-C7-环烷基-低级烷基、芳基-低级烷基、双芳基-低级烷基、低级烷氧基、芳基-低级烷氧基、芳氧基、N-低级烷基氨基、N,N-二低级烷基氨基、N-芳基-低级烷基氨基、N,N-二芳基-低级烷基氨基、N-芳基氨基、N,N-二芳基氨基、低级烷酰氨基、芳基-低级烷酰氨基或芳基氨基；R2 代表氢、羟基、低级烷氧基、低级烷基、芳基-低级烷基、C3-C7-环烷基-低级烷基、氨基-低级烷基、羟基-低级烷基、低级烷硫基-低级烷基、低级烷氧基-低级烷基、芳基-低级烷硫基-低级烷基或芳基-低级烷氧基-低级烷基；双芳基代表被碳环或杂环芳基取代的苯基；A 代表直接键、低级亚烷基、亚苯基或环己基；m 代表 1 或 0，但当 A 为直接键时，m 代表 1；或其药学上可接受的盐；包含所述化合物的药物组合物；制备所述化合物和制备中间体的方法；以及通过向需要治疗的哺乳动物施用所述化合物来治疗对中性内肽酶的抑制有反应的哺乳动物疾病的方法。
• METHOD FOR SYNTHESIZING OPTICALLY ACTIVE -AMINO ACID USING CHIRAL METAL COMPLEX COMPRISING AXIALLY CHIRAL N-(2-ACYLARYL)-2-[5,7-DIHYDRO-6H-DIBENZO[c,e]AZEPIN-6-YL]ACETAMIDE COMPOUND AND AMINO ACID
  申请人：Hamari Chemicals, Ltd.

  公开号：EP3006449A1

  公开（公告）日：2016-04-13

  Objects of the present invention are to provide an industrially applicable method for producing an optically active α-amino acid in high yield and in a highly enantioselective manner, to provide a simple production method of an optically active α,α-disubstituted α-amino acid, and to provide an intermediate useful for the above production methods of an optically active α-amino acid and an optically active α,α-disubstituted α-amino acid. The present invention provides a production method of an optically active α-amino acid or a salt thereof, the production method comprising introducing a substituent into the α carbon in the α-amino acid moiety of a metal complex represented by the following Formula (1): by an alkylation reaction, an aldol reaction, the Michael reaction, or the Mannich reaction, and releasing an optically pure α-amino acid enantiomer or a salt thereof by acid decomposition of the metal complex.

  本发明的目的是提供一种工业上适用的高产率和高对映选择性生产光学活性α-氨基酸的方法，提供一种光学活性α,α-二取代α-氨基酸的简单生产方法，以及提供一种对上述光学活性α-氨基酸和光学活性α,α-二取代α-氨基酸生产方法有用的中间体。 本发明提供了一种光学活性α-氨基酸或其盐的生产方法，该生产方法包括在下式（1）表示的金属配合物的α-氨基酸分子中的α碳上引入取代基： 通过烷基化反应、醛醇反应、迈克尔反应或曼尼希反应，并通过酸分解金属络合物释放出光学纯的α-氨基酸对映体或其盐。