1-(N-benzyloxycarbonyl-glycyl)-DL-proline | 68047-33-6

• 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: 1-(N-benzyloxycarbonyl-glycyl)-DL-proline
• 英文别名: 1-(N-Benzyloxycarbonyl-glycyl)-DL-prolin；1-{N-[(phenylmethoxy)carbonyl]glycyl}-DL-proline；Carbobenzoxyglycyl-L-proline；1-[2-(phenylmethoxycarbonylamino)acetyl]pyrrolidine-2-carboxylic acid
• CAS: 68047-33-6
• 化学式: C₁₅H₁₈N₂O₅
• mdl: MFCD01096309
• 分子量: 306.318
• InChiKey: ZTUKZKYDJMGJDC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  22
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  95.9
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  1-(N-benzyloxycarbonyl-glycyl)-DL-proline 在 甲醇 、 钯 、 溶剂黄146 作用下， 生成 1-glycyl-DL-proline ethyl ester; hydrochloride
  参考文献：
  名称：

  702.多肽。第四部分 甘氨酸和脯氨酸某些肽的酯的自缩合

  摘要：

  DOI：

  10.1039/jr9560003642
• 作为产物：
  描述：

  tert-butyl 1-(((benzyloxy)carbonyl)glycyl)-5-oxopyrrolidine-2-carboxylate 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 生成 1-(N-benzyloxycarbonyl-glycyl)-DL-proline
  参考文献：
  名称：

  [EN] TEAD INHIBITORS
  [FR] INHIBITEURS DE TEAD

  摘要：

  The present invention relates to a compound of formula (I) wherein A, Z, L, R1, R2, R3, R4, R5and R33are as defined in claim 1, or a pharmaceutically acceptable salt thereof. The compounds of formula (I) possess utility as inhibitors of TEAD. The compounds are useful as medicaments in the treatment of diseases or conditions wherein inhibition of TEAD is desired, such as cancer and chronic pain.

  公开号：

  WO2022219246A1

文献信息

• Decarboxylative Alkynylation and Cyanation of Carboxylic Acids using Photoredox Catalysis and Hypervalent Iodine Reagents
  作者：Franck Le Vaillant、Jérôme Waser

  DOI：10.2533/chimia.2017.226

  日期：——

  in material and medicinal sciences. A convenient and straightforward access to both classes of compounds under mild conditions is, therefore, highly desirable. Herein, we disclose the decarboxylative alkynylation and cyanation of broadly available carboxylic acids using photoredox catalysis and hypervalent iodine reagents. Choices of both catalysts and reagents were crucial. Computational and experimental

  炔烃和腈是重要的官能团，可作为有机合成中的通用构建基块，并在材料和药物科学中得到应用。因此，非常需要在温和条件下方便且直接地获得两类化合物。在此，我们公开了使用光氧化还原催化和高价碘试剂对广泛可用的羧酸进行脱羧炔基化和氰化反应。催化剂和试剂的选择至关重要。计算和实验研究揭示了由试剂的氧化电位决定的两种不同的可能机理：自由基用于炔基化，离子用于氰化。
• [EN] NEAR INFRA-RED MOLECULAR PROBES FOR USE IN DIAGNOSIS OF FIBROTIC CONDITIONS AND SCREENING OF ANTI-FIBROTIC DRUGS<br/>[FR] SONDES MOLÉCULAIRES EN PROCHE INFRAROUGE DESTINÉES À ÊTRE UTILISÉES DANS LE DIAGNOSTIC DE TROUBLES FIBROTIQUES ET LE CRIBLAGE DE MÉDICAMENTS ANTI-FIBROTIQUES
  申请人：UNIV NANYANG TECH

  公开号：WO2019117812A1

  公开（公告）日：2019-06-20

  We disclose a compound of formula I: [X]n-[Y]m-Z where X represents a fluorophore group covalently linked to the rest of the molecule by way of an oxygen atom or an NH group; Y is a self-immolative linking group; Z represents an N-blocked dipeptide Gly-Pro; n is 1 -2; and m is 0-1. The fluorophore X does not fluoresce when attached to the rest of the molecule by way of a covalent bond, but is capable of fluorescence following cleavage of said covalent bond. The compounds of formula I are useful as a fluorescent probe in the diagnosis of fibrotic conditions in vivo, such as keloidal and/or hypertrophic scarring, and may also be used in an in vitro test to screen for compounds useful to treat such fibrotic conditions. Also disclosed herein is the use of RepSox and thiazovivin, whether alone or in combination, to treat fibrotic conditions.

  我们披露了一种具有化学式I的化合物：[X]n-[Y]m-Z，其中X代表与分子其余部分通过氧原子或NH基共价连接的荧光团；Y是自灭联结基团；Z代表N-阻断二肽甘氨酸-脯氨酸；n为1-2；m为0-1。荧光团X在通过共价键连接到分子其余部分时不发出荧光，但在断开该共价键后能够发出荧光。化学式I的化合物可用作体内纤维化疾病的诊断荧光探针，例如瘢痕性和/或肥厚性瘢痕，并且还可用于体外试验以筛选用于治疗这些纤维化疾病的化合物。本文还披露了使用RepSox和thiazovivin，无论是单独使用还是结合使用，来治疗纤维化疾病。
• VINBLASTINE DERIVATIVES, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
  申请人：JINAN UNIVERSITY

  公开号：US20160068552A1

  公开（公告）日：2016-03-10

  The present invention provides a new kind of vinca alkaloid derivatives, new applications thereof and preparation methods therefor. The vinca alkaloid derivatives comprise hydrazinolyzed vinca alkaloids and vinca alkaloid dipeptide derivative. The hydrazinolyzed vinca alkaloids are the compounds obtained from the reaction of vinca alkaloids or salts thereof with hydrazinolyzed hydrate; and the vinca alkaloid dipeptide derivatives are the compounds obtained from the condensation of hydrazinolyzed vinca alkaloids with N-benzyloxycarbonylglycyl proline. The present invention provides the uses of the vinca alkaloids derivatives or the pharmaceutical compositions thereof in anti-tumor, preventing or treating diabetic retinopathy, rheumatoid arthritis and serving as angiogenesis inhibitors or vascular disrupting agents.

  本发明提供了一种新型的长春碱衍生物，以及其新的应用和制备方法。长春碱衍生物包括水解长春碱和长春碱二肽衍生物。水解长春碱是通过长春碱或其盐与水解水合物反应得到的化合物；而长春碱二肽衍生物是通过水解长春碱与N-苄氧羰基甘氨酸脯氨酸的缩合反应得到的化合物。本发明提供了长春碱衍生物或其药物组合物在抗肿瘤、预防或治疗糖尿病视网膜病变、类风湿性关节炎以及作为血管生成抑制剂或血管破坏剂中的用途。
• Vinblastine derivatives, preparation method therefor and application thereof
  申请人：JINAN UNIVERSITY

  公开号：US10377774B2

  公开（公告）日：2019-08-13

  The present invention provides a new kind of vinca alkaloid derivatives, new applications thereof and preparation methods therefor. The vinca alkaloid derivatives comprise hydrazinolyzed vinca alkaloids and vinca alkaloid dipeptide derivative. The hydrazinolyzed vinca alkaloids are the compounds obtained from the reaction of vinca alkaloids or salts thereof with hydrazinolyzed hydrate; and the vinca alkaloid dipeptide derivatives are the compounds obtained from the condensation of hydrazinolyzed vinca alkaloids with N-benzyloxycarbonylglycyl proline. The present invention provides the uses of the vinca alkaloids derivatives or the pharmaceutical compositions thereof in anti-tumor, preventing or treating diabetic retinopathy, rheumatoid arthritis and serving as angiogenesis inhibitors or vascular disrupting agents.

  本发明提供了一种新的长春花生物碱衍生物、其新的应用及其制备方法。长春花生物碱衍生物包括肼解长春花生物碱和长春花生物碱二肽衍生物。肼解长春花生物碱是长春花生物碱或其盐与肼解水合物反应得到的化合物；长春花生物碱二肽衍生物是肼解长春花生物碱与 N-苄氧羰基甘氨酰脯氨酸缩合得到的化合物。本发明提供了长春花生物碱衍生物或其药物组合物在抗肿瘤、预防或治疗糖尿病视网膜病变、类风湿性关节炎以及作为血管生成抑制剂或血管破坏剂中的用途。
• [EN] VINBLASTINE DERIVATIVES, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF<br/>[FR] DÉRIVÉS DE VINBLASTINE, LEUR PROCÉDÉ DE SYNTHÈSE ET LEUR APPLICATION
  申请人：UNIV JINAN

  公开号：WO2014169697A1

  公开（公告）日：2014-10-23

  本发明提供一类新的长春碱类衍生物及其新应用和制备方法。所述长春碱类衍生物包括肼解长春碱类化合物和长春碱类二肽衍生物。所述的肼解长春碱类化合物为长春碱类化合物或其盐与水合肼反应所得到的化合物；所述的长春碱类二肽衍生物为肼解长春碱类化合物与N−苄氧羰基甘氨酰脯氨酸缩合所得的化合物。本发明提供了所述长春碱类衍生物或其药物组合在抗肿瘤、预防或治疗糖尿病性视网膜病变、类风湿关节炎以及作为血管生成抑制剂或者血管阻断剂中的用途。