(E)-3-(4-aminophenyl)prop-2-en-1-ol

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 肉桂醇
• 英文名称: (E)-3-(4-aminophenyl)prop-2-en-1-ol
• 英文别名: 4-aminocinnamyl alcohol
• 化学式: C₉H₁₁NO
• 分子量: 149.192
• InChiKey: WQXGKIRAARPVJD-OWOJBTEDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  46.2
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (E)-3-(4-aminophenyl)prop-2-en-1-ol 、 二碳酸二叔丁酯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 以82%的产率得到tert-butyl (E)-(4-(3-hydroxyprop-1-en-1-yl)phenyl)carbamate
  参考文献：
  名称：

  开环复分解和区域选择性链转移的杂多烯聚合物

  摘要：

  杂多烯聚合物是通过动力学远螯开环复分解聚合方法合成的，该方法依靠正在传播的Grubbs第一代催化剂与肉桂醇衍生物的区域选择性交叉复分解。该程序允许一锅法合成杂双端功能聚合物。可以通过改变肉桂醇衍生物与单体之间的比例来控制聚合物的分子量。可以使用不同的芳族取代肉桂醇衍生物来改变末端官能团。研究了不同的单体，并通过NMR光谱和MALDI-ToF质谱法显示了官能团的存在。

  DOI：

  10.1002/anie.201708733
• 作为产物：
  描述：

  (2E)-3-(4-氨基苯基)-2-丙烯酸 在 sodium borohydrid 作用下， 以 甲醇 为溶剂， 生成 (E)-3-(4-aminophenyl)prop-2-en-1-ol
  参考文献：
  名称：

  CNS active compounds

  摘要：

  式为##STR1##的化合物，其中R可以是氢或由1至10个碳原子的直链或支链烷基基团，由6至10个碳原子的芳基，或由7至10个碳原子的芳基烷基；Y可以是氢，由1至4个碳原子的烷基，CF.sub.3，F，Cl或Br；Z可以是氢或如下所定义的。这些化合物可用作中枢神经系统兴奋剂，更具体地用于增强表现或作为情绪提升剂。

  公开号：

  US04022897A1

文献信息

• Yeast supported gold nanoparticles: an efficient catalyst for the synthesis of commercially important aryl amines
  作者：Saravanan Krishnan、Paresh N. Patel、Kalpattu K. Balasubramanian、Anju Chadha

  DOI：10.1039/d0nj04542j

  日期：——

  and substituted nitroarenes with different functional groups like halides (–F, –Cl, –Br), olefins, esters and nitriles using sodium borohydride. The product aryl amines which are useful for the preparation of pharmaceuticals, polymers and agrochemicals were obtained in good yields (up to >95%) using CpGNP catalyst under mild conditions. The catalyst showed high recyclability (≥10 cycles) and is a robust

  通过简单，绿色的方法制备的假丝酵母假单胞菌ATCC 7330支持的金纳米粒子（CpGNP）可以使用硼氢化钠选择性还原具有不同官能团（例如卤化物（-F，-Cl，-Br），烯烃，酯和腈）的硝基芳烃和取代的硝基芳烃。使用CpGNP催化剂，在温和的条件下，以良好的收率（高达95％以上）获得了用于制备药物，聚合物和农用化学品的芳基胺产物。该催化剂显示出很高的可回收性（≥10个循环），并且是一种坚固的自由流动性粉末，八个月后可以储存和使用，而催化活性没有任何损失。
• Elongated and multiple spacers containing activatible prodrugs
  申请人：De Groot, Franciscus Marinus Hendrikus

  公开号：EP1243276A1

  公开（公告）日：2002-09-25

  This invention is directed to prodrugs that can be activated at the preferred site of action in order to selectively deliver the corresponding therapeutic parent drugs to target cells or to the target site. This invention will therefore primarily but not exclusively relate to tumor cells as target cells. More specifically the prodrugs are compounds of the formula V-(W)k-(X)l-A-Z, wherein: V is a specifier; W and X are each a 1, (4+2n) electronic cascade spacer, being the same or different; A is either a spacer group of formula (Y)m, wherein: Y is a 1, (4+2n) electronic cascade spacer, or a group of formula U being a cyclisation elimination spacer; Z is a therapeutic drug; k, l and m are integers from 0 to 5; n is an integer of 0 to 10, with the provisos that: when A is (Y)m: k+l+m > 1, and if k+l+m=1, then n > 1; when A is U: k+l > 1.

  本发明涉及一种前药，可以在首选作用部位被激活，以有选择性地将相应的治疗母药物送达目标细胞或目标部位。因此，本发明主要但不仅限于与肿瘤细胞作为靶细胞相关。更具体地说，所述前药是化合物V-(W)k-(X)l-A-Z，其中：V是一个指示符；W和X分别是1，（4+2n）电子级联间隔物，可以相同也可以不同；A是公式（Y）m的间隔基，其中：Y是1，（4+2n）电子级联间隔物，或者是公式U的基团，是一个环化消除间隔物；Z是治疗药物；k、l和m是0至5的整数；n是0至10的整数，但是必须满足以下条件：当A是（Y）m时：k+l+m>1，如果k+l+m=1，则n>1；当A是U时：k+l>1。
• [EN] ELONGATED AND MULTIPLE SPACERS IN ACTIVATIBLE PRODRUGS<br/>[FR] ESPACEURS ALLONGES ET MULTIPLES DE PRODROGUES ACTIVABLES
  申请人：DE GROOT FRANCISCUS MARINUS HE

  公开号：WO2002083180A1

  公开（公告）日：2002-10-24

  This invention is directed to prodrugs that can be activated at the preferred site of action in order to selectively deliver the corresponding therapeutic parent drugs to target cells or to the target site. This invention will therefore primarily but not exclusively relate to tumor cells as target cells. More specifically the prodrugs are compounds of the formula V-(W)k-(X)1-A-Z, wherein: V is a specifier; (W)k-(X)1-A is an elongated self-elimination spacer system; W and X are each a 1,(4+2n) electronic cascade spacer, being the same or different; A is either a spacer group of formula (Y)m wherein: Y is a 1,(4+2n) electronic cascade spacer, or a group of formula U being a cyclisation elimination spacer; Z is a therapeutic drug; k, 1 and m are integers from 0 (included) to 5 (included); n is an integer of 0 (included) to 10 (included), with the provisos that: - when A is (Y)m: k+1+m ≥ 1, and if k+1+m = 1; - when A is U: k+1 ≥ 1.

  本发明涉及一种前药，可以在首选作用部位激活，以有选择地将相应的治疗母药物传递到目标细胞或目标部位。因此，本发明主要但不仅限于将肿瘤细胞作为目标细胞。更具体地，前药是化合物V-(W)k-(X)1-A-Z，其中：V是说明符；(W)k-(X)1-A是一个延长的自我消除间隔系统；W和X分别是1，（4+2n）电子级联间隔器，相同或不同；A是公式（Y）m的间隔基团，其中：Y是1，（4+2n）电子级联间隔器，或者是公式U的基团，是环化消除间隔器；Z是治疗药物；k，1和m是从0（包括）到5（包括）的整数；n是0（包括）到10（包括）的整数，但前提是：当A为（Y）m时：k+1+m≥1，如果k+1+m=1；当A为U时：k+1≥1。
• Elongated and multiple spacers in activatible produgs
  申请人：——

  公开号：US20040121940A1

  公开（公告）日：2004-06-24

  This invention is directed to prodrugs that can be activated at the preferred site of action in order to selectively deliver the corresponding therapeutic parent drugs to target cells or to the target site. This invention will therefore primarily but not exclusively relate to tumor cells as target cells. More specifically the prodrugs are compounds of the formula V—(W)k-(X)l-A-Z, wherein: V is a specifier; (W)k-(X)l-A is an elongated self-elimination spacer system; W and X are each a l,(4+2n) electronic cascade spacer, being the same or different; A is either a spacer group of formula (Y) m wherein: Y is a l,(4+2n) electronic cascade spacer, or a group of formula U being a cyclisation elimination spacer; Z is a therapeutic drug; k, l and m are integers from 0 (included) to 5 (included); n is an integer of 0 (included) to 10 (included), with the provisos that:—when A is (Y)m: k+l+m 1, and if k+l+m=1;—when A is U: k+l 1.

  本发明涉及一种前药，可以在优选的作用部位被激活，以有选择地将相应的治疗原药物递送到靶细胞或靶部位。因此，本发明主要但不仅限于与肿瘤细胞作为靶细胞相关。更具体地说，前药是公式V—(W)k-(X)l-A-Z的化合物，其中：V是说明符；(W)k-(X)l-A是一个延长的自我消除间隔系统；W和X分别是l，（4+2n）电子级联间隔器，可以相同也可以不同；A是公式（Y）m的间隔基，其中：Y是l，（4+2n）电子级联间隔器，或者是公式U的基团，是一个环化消除间隔器；Z是治疗药物；k、l和m是从0（包括）到5（包括）的整数；n是0（包括）到10（包括）的整数，但限制条件是：当A是（Y）m时：k+l+m≥1，如果k+l+m=1；当A是U时：k+l≥1。
• B7-H3 binding molecules, antibody drug conjugates thereof and methods of use thereof
  申请人：MacroGenics, Inc.

  公开号：US10961311B2

  公开（公告）日：2021-03-30

  The present invention is directed to novel B7-H3-binding molecules capable of binding to human and non-human B7-H3, and in particular to such molecules that are cross-reactive with B7-H3 of a non-human primate (e.g., a cynomolgus monkey). The invention additionally pertains to B7-H3-binding molecules that comprise Variable Light Chain and/or Variable Heavy Chain (VH) Domains that have been humanized and/or deimmunized so as to exhibit a reduced immunogenicity upon administration to recipient subjects. The invention particularly pertains to bispecific, trispecific or multispecific B7-H3-binding molecules, including bispecific diabodies, BiTEs, bispecific antibodies, trivalent binding molecules, etc. that comprise: (i) such B7-H3-binding Variable Domains and (ii) a domain capable of binding to an epitope of a molecule present on the surface of an effector cell. The invention is also directed to pharmaceutical compositions that contain any of such B7-H3-binding molecules, and to methods involving the use of any of such B7-H3-binding molecules in the treatment of cancer and other diseases and conditions. The invention also particularly pertains to a molecule that comprises the human B7-H3 binding domain of a humanized anti-human B7-H3 antibody conjugated to at least one drug moiety (a “B7-H3-ADC”). The invention is also directed to pharmaceutical compositions that contain such B7-H3-ADCs, and to methods involving the use of any of such B7-H3-ADCs in the treatment of cancer and other diseases and conditions.

  本发明涉及能够与人类和非人类 B7-H3 结合的新型 B7-H3 结合分子，特别是与非人灵长类动物（如猕猴）的 B7-H3 具有交叉反应的分子。此外，本发明还涉及包含可变轻链和/或可变重链（VH）域的 B7-H3 结合分子，这些分子已被人源化和/或去免疫化，以便在给受试者用药时显示出较低的免疫原性。本发明尤其涉及双特异性、三特异性或多特异性 B7-H3 结合分子，包括双特异性二抗体、双特异性抗体、双特异性抗体、三价结合分子等，这些分子包含：(i) 这种 B7-H3 结合可变区；(ii) 能够与效应细胞表面存在的分子表位结合的结构域。本发明还涉及含有任何此类 B7-H3 结合分子的药物组合物，以及涉及使用任何此类 B7-H3 结合分子治疗癌症及其他疾病和病症的方法。本发明还特别涉及一种分子，该分子包括与至少一种药物分子（"B7-H3-ADC"）共轭的人源化抗人 B7-H3 抗体的人 B7-H3 结合域。本发明还涉及含有此类 B7-H3-ADC 的药物组合物，以及涉及使用任何此类 B7-H3-ADC 治疗癌症及其他疾病和病症的方法。