3-Amino-2,2-dimethylbutanoic acid | 720660-14-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 3-Amino-2,2-dimethylbutanoic acid
• CAS: 720660-14-0
• 化学式: C₆H₁₃NO₂
• 分子量: 131.17
• InChiKey: JQRDIZQROJQBDM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.1
• 重原子数：
  9
• 可旋转键数：
  2
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  63.3
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• BETA-AMINO ACIDS AND METHODS AND INTERMEDIATES FOR MAKING SAME
  申请人：Sibi Mukund P.

  公开号：US20110218342A1

  公开（公告）日：2011-09-08

  Disclosed are β-amino acids that are unsubstituted in the β position; that are substituted in the β position with an aryl group; that are substituted in the α position with an aryl group; that bear two substituents in the α position; and/or that are substituted in the α and β positions with groups which, together with the carbon atoms at the α and β positions, form a ring. Also disclosed are methods for making the above-mentioned β-amino acids and other β-amino acids which involve providing an α,β-unsaturated imide; converting the α,β-unsaturated imide to a 2-substituted-isoxazolidin-5-one; and converting the 2-substituted-isoxazolidin-5-one to a β-amino acid.

  披露了未在β位取代的β-氨基酸；在β位用芳基取代的β-氨基酸；在α位用芳基取代的β-氨基酸；在α位带有两个取代基的β-氨基酸；和/或在α和β位用与α和β位的碳原子一起形成环的基团取代的β-氨基酸。还披露了制备上述β-氨基酸和其他β-氨基酸的方法，包括提供α，β-不饱和亚胺；将α，β-不饱和亚胺转化为2-取代异噁唑啉-5-酮；将2-取代异噁唑啉-5-酮转化为β-氨基酸。
• [EN] NOVEL CRYPTOPHYCIN COMPOUNDS AND CONJUGATES, THEIR PREPARATION AND THEIR THERAPEUTIC USE<br/>[FR] NOUVEAUX COMPOSÉS ET CONJUGUÉS DE CRYPTOPHYCINE, LEUR PRÉPARATION ET LEUR UTILISATION THÉRAPEUTIQUE
  申请人：SANOFI SA

  公开号：WO2017076998A1

  公开（公告）日：2017-05-11

  The present invention relates to cryptophycin compounds of formula (I). The invention also relates to cryptophycin payloads, to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The invention also relates to the process for preparing these conjugates.

  本发明涉及公式（I）的隐藻素化合物。该发明还涉及隐藻素有效载荷、隐藻素偶联物、含有它们的组合物及其治疗用途，尤其是作为抗癌剂。该发明还涉及制备这些偶联物的过程。
• Novel process for the preparation of 6,7-Diacyl-7-deacetylforskolin derivatives
  申请人：NIPPON KAYAKU KABUSHIKI KAISHA

  公开号：EP0297496A2

  公开（公告）日：1989-01-04

  This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: wherein R¹ and R² each stands for an acyl group and R³ stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: wherein R¹, R² and R³ are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.

  本发明涉及一种由通式表示的 6,7-二乙酰基-7-脱乙酰基佛司可林衍生物的制备方法： 其中R¹和R²分别代表一个酰基，R³代表一个具有2至3个碳原子的脂肪族基团，该工艺包括消除通式为1,6,7-三酰基-7-脱乙酰基佛司可林衍生物中位于位置1的酰基： 其中 R¹、R² 和 R³ 如上定义，通过溶解作用。式 (I) 的化合物预期为药物。
• Cryptophycin compounds and conjugates, their preparation and their therapeutic use
  申请人：SANOFI

  公开号：US10941139B2

  公开（公告）日：2021-03-09

  The present invention relates to cryptophycin compounds of formula (I). The invention also relates to cryptophycin payloads, to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The invention also relates to the process for preparing these conjugates.

  本发明涉及式（I）的隐球霉素化合物。本发明还涉及隐球菌苷有效载荷、隐球菌苷共轭物、含有它们的组合物及其治疗用途，特别是作为抗癌剂。本发明还涉及制备这些共轭物的工艺。
• [DE] NEUES VERFAHREN ZUR HERSTELLUNG VON NORBENZOMORPHAN EINER ZWISCHENSTUFE BEI HERSTELLUNG VON PHARMAZEUTISCH WERTVOLLEN BENZOMORPHANDERIVATEN, INSBESONDERE VON (-)-(1R,5S,2"R)-3'-HYDROXY-2-(2-METHOXYPROPYL)-5,9,9-TRIMETHYL-6,7-BENZOMORPHAN<br/>[EN] METHOD OF PREPARING NORBENZOMORPHANE AS AN INTERMEDIATE IN THE PREPARATION OF PHARMACEUTICALLY USEFUL BENZOMORPHANE DERIVATIVES, IN PARTICULAR (-)-(1R,5S,2"R)-3'-HYDROXY-2-(2-METHOXYPROPYL)-5,9,9-TRIMETHYL-6,7-BENZOMORPHANE<br/>[FR] NOUVEAU PROCEDE DE PREPARATION DE NORBENZOMORPHANE D'UN INTERMEDE LORS DE LA PREPARATION DE DERIVES DE BENZOMORPHANE INTERESSANTS SUR LE PLAN PHARMACEUTIQUE, NOTAMMENT DE (-)-(1R,5S,2"R)-3'-HYDROXY-2-(2-METHOXYPROPYLE)-5,9,9-TRIMETHYLE-6,7-BENZOMORPHANE
  申请人：BOEHRINGER INGELHEIM KG

  公开号：WO1997006146A1

  公开（公告）日：1997-02-20

  (DE) Die vorliegende Erfindung betrifft ein neues Verfahren zur Herstellung von Norbenzomorphan - der zentralen Zwischenstufe bei der Herstellung von pharmazeutisch wertvollen Benzomorphanderivaten der allgemeinen Formel (1), insbesondere von (-)-(1R,5S,2'R)-3'-Hydroxy-2-(2-methoxypropyl)-5,9,9-trimethyl-6,7-benzomorphan bzw. [(-)-(2R,6S,2'R)-3-(2-Methoxypropyl)-6,11,11-trimethyl-1,2,3,4,5,6-hexahydro-2,6-methano-benzo[$g(a)]oxacin-9-ol] (BIII 277).(EN) The invention concerns a method of preparing norbenzomorphane in the central intermediate stage in the preparation of pharmaceutically useful benzomorphane derivatives of general formula (1), in particular (-)-(1R,5S,2'R)-3'-hydroxy-2-(2-methoxypropyl)-5,9,9-trimethyl-6,7-benzomorphane or [(-)-(2R,6S,2'R)-3-(2-methoxypropyl)-6,11,11-trimethyl-1,2,3,4,5,6-hexahydro-2,6-methanobenzo[$g(a)]oxacin-9-ol] (BIII 277).(FR) L'invention concerne un nouveau procédé de préparation de norbenzomorphane de l'intermède central, lors de la préparation de dérivés de benzomorphane de la formule générale (1) intéressants sur le plan pharmaceutique, notamment de (-)-(1R,5S,2'R)-3'-hydroxy-2-(2-méthoxypropyle)-5,9,9-triméthyle-6,7-benzomorphane ou [(-)-2R,6S,2'R)-3-(2-méthoxypropyle)-6,11,11-triméthyle-1,2,3,4,5,6-hexahydro-2,6-méthano-benzo[$g(a)]oxacine-9-ol] (BIII 277).

  这项发明涉及一种新的合成方法用于制备Norb Azomorphane，特别是中间体阶段，在 pharmaceutically valuable benzomorphane derivatives 的合成中，其通用化学式为（1）。尤其是在制备具有特定立体化学的化合物，例如（-）-(1R,5S,2'R)-3'-羟基-2-(2-甲氧丙基)-5,9,9-三角甲基-6,7-azetidine-7-甲基-2（S）-、3（R）-的位置的 benzomorphane，或者[（-）-2R,6S,2'R)-3-(2-甲氧丙基)-6,11,11-三角甲基-1,2,3,4,5,6-六氢甲基-2,6-双甲基-oxacine-9-ol]（BIII 277）。