N-benzyl-N-methyl-N-(2-methylindolizin-1-yl)amine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: N-benzyl-N-methyl-N-(2-methylindolizin-1-yl)amine
• 英文别名: N-benzyl-N,2-dimethylindolizin-1-amine
• 化学式: C₁₇H₁₈N₂
• 分子量: 250.343
• InChiKey: DPRSICXTIPVBPS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  7.6
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  N-benzyl-N-methyl-1-(pyridin-2-yl)methanamine 、 一氯丙酮 以970 mg of a yellow oil are obtained的产率得到N-benzyl-N-methyl-N-(2-methylindolizin-1-yl)amine
  参考文献：
  名称：

  Novel 1,2,3-Substituted Indolizine Derivatives, Inhibitors of FGFs, Method for Preparing Them and Pharmaceutical Compositions Containing Them

  摘要：

  本发明涉及新型1,2,3-取代吲哚嗪衍生物，它们是成纤维细胞生长因子的抑制剂，涉及制备这种衍生物的方法，涉及包含这种衍生物的制药组合物，以及涉及使用这种衍生物的治疗方法。

  公开号：

  US20090023770A1

文献信息

• Novel 1,2,3-substituted indolizine derivatives, inhibitors of fgfs, method for making same and pharmaceutical compositions containing same
  申请人：Badorc Alain

  公开号：US20050203126A1

  公开（公告）日：2005-09-15

  Compounds of formula I or salts thereof: in which R 1 represents —OH, (C 1 -C 5 )alkoxy, carboxyl, (C 2 -C 6 )alkoxycarbonyl, —NR 5 R 6 , —NH—SO 2 -Alk, —NH—SO 2 -Ph, —NH—CO-Ph, —N(Alk)-CO-Ph, —NH—CO—NH-Ph, —NH—CO-Alk, —NH—CO 2 -Alk, —O—(CH 2 ) n -cAlk, —O-Alk-COOR 7 , —O-Alk-O—R 8 , —O-Alk-OH, —O-Alk-C(NH 2 ):NOH, —O-Alk-NR 5 R 6 , —O-Alk-CN, —O—(CH 2 ) n -Ph, —O-Alk-CO—NR 5 R 6 , —CO—NH—(CH 2 ) m —COOR 7 , —CO—NH-Alk R 2 represents H, (C 1 -C 5 )alkyl, (C 1 -C 5 )alkyl halide, (C 3 -C 6 )cycloalkyl or phenyl which is optionally substituted, A represents —CO—, —SO— or —SO 2 —, R 3 and R 4 which are identical or different, each represent H, (C 1 -C 5 )alkoxy, amino, carboxyl, (C 2 -C 6 )alkoxycarbonyl, —OH, nitro, hydroxyamino, -Alk-COOR 7 , —NR 5 R 6 , —NH-Alk-COOR 7 , —NH—COO-Alk, —N(R 11 )—SO 2 -Alk-NR 9 R 10 , —N(R 11 )—SO 2 -Alk, —N(R 11 )-Alk-NR 5 R 6 , —N(R 11 )—CO-Alk-NR 9 R 10 , —N(R 11 )—CO-Alk, —N(R 11 )—CO—CF 3 , —NH-Alk-HetN, —O-Alk-NR 9 R 10 , —O-Alk-CO—NR 5 R 6 , —O-Alk-HetN, or R 3 and R 4 form together a 5- to 6-membered unsaturated heterocycle, are inhibitors of basic fibroblast growth factors.

  化学式I或其盐的化合物：其中R1代表—OH，(C1-C5)烷氧基，羧基，(C2-C6)烷氧羰基，—NR5R6，—NH—SO2-Alk，—NH—SO2-Ph，—NH—CO-Ph，—N(Alk)-CO-Ph，—NH—CO—NH-Ph，—NH—CO-Alk，—NH—CO2-Alk，—O—(CH2)n-烷基，—O-Alk-COOR7，—O-Alk-O—R8，—O-Alk-OH，—O-Alk-C(NH2):NOH，—O-Alk-NR5R6，—O-Alk-CN，—O—( )n-Ph，—O-Alk-CO—NR5R6，—CO—NH—( )m—COOR7，—CO—NH-AlkR2代表H，(C1-C5)烷基，(C1-C5)烷基卤化物，(C3-C6)环烷基或苯基，可选择性地取代，A代表—CO—，—SO—或—SO2—，R3和R4相同或不同，各自代表H，(C1-C5)烷氧基，氨基，羧基，(C2-C6)烷氧羰基，—OH，硝基，羟胺基，-Alk-COOR7，—NR5R6，—NH-Alk-COOR7，—NH—COO-Alk，—N(R11)—SO2-Alk-NR9R10，—N(R11)—SO2-Alk，—N(R11)-Alk-NR5R6，—N(R11)—CO-Alk-NR9R10，—N(R11)—CO-Alk，—N(R11)—CO—CF3，—NH-Alk-HetN，—O-Alk-NR9R10，—O-Alk-CO—NR5R6，—O-Alk-HetN，或R3和R4共同形成5-至6-成员不饱和杂环，是基本成纤维细胞生长因子的抑制剂。
• 1,2,3-substituted indolizine derivatives, inhibitors of fgfs, method for making same and pharmaceutical compositions containing same
  申请人：Sanofi-Aventis

  公开号：US07442708B2

  公开（公告）日：2008-10-28

  Compounds of formula I or salts thereof: in which R1 represents —OH, (C1-C5)alkoxy, carboxyl, (C2-C6)alkoxycarbonyl, —NR5R6, —NH—SO2-Alk, —NH—SO2-Ph, —NH—CO-Ph, —N(Alk)-CO-Ph, —NH—CO—NH-Ph, —NH—CO-Alk, —NH—CO2-Alk, —O—(CH2)n-cAlk, —O-Alk-COOR7, —O-Alk-O—R8, —O-Alk-OH, —O-Alk-C(NH2):NOH, —O-Alk-NR5R6, —O-Alk-CN, —O—(CH2)n-Ph, —O-Alk-CO—NR5R6, —CO—NH—(CH2)m—COOR7, —CO—NH-Alk R2 represents H, (C1-C5)alkyl, (C1-C5)alkyl halide, (C3-C6)cycloalkyl or phenyl which is optionally substituted, A represents —CO—, —SO— or —SO2—, R3 and R4 which are identical or different, each represent H, (C1-C5)alkoxy, amino, carboxyl, (C2-C6)alkoxycarbonyl, —OH, nitro, hydroxyamino, -Alk-COOR7, —NR5R6, —NH-Alk-COOR7, —NH—COO-Alk, —N(R11)—SO2-Alk-NR9R10, —N(R11)—SO2-Alk, —N(R11)-Alk-NR5R6, —N(R11)—CO-Alk-NR9R10, —N(R11)—CO-Alk, —N(R11)—CO—CF3, —NH-Alk-HetN, —O-Alk-NR9R10, —O-Alk-CO—NR5R6, —O-Alk-HetN, or R3 and R4 form together a 5- to 6-membered unsaturated heterocycle, are inhibitors of basic fibroblast growth factors.

  化合物I的公式或其盐： 其中 R1代表-OH，(C1-C5)烷氧基，羧基，(C2-C6)烷氧羰基，-NR5R6，-NH-SO2-Alk，-NH-SO2-Ph，-NH-CO-Ph，-N（Alk）-CO-Ph，-NH-CO-NH-Ph，-NH-CO-Alk，-NH-CO2-Alk，-O-(CH2)n-烷基，-O-Alk-COOR7，-O-Alk-O-R8，-O-Alk-OH，-O-Alk-C（NH2）：NOH，-O-Alk-NR5R6，-O-Alk-CN，-O-( )n-Ph，-O-Alk-CO-NR5R6，-CO-NH-( )m-COOR7，-CO-NH-Alk R2代表H，(C1-C5)烷基，(C1-C5)烷基卤代，(C3-C6)环烷基或苯基，可选地取代 A代表-CO-，-SO-或-SO2- R3和R4相同或不同，每个代表H，(C1-C5)烷氧基，氨基，羧基，(C2-C6)烷氧羰基，-OH，硝基，羟基氨基，-Alk-COOR7，-NR5R6，-NH-Alk-COOR7，-NH-COO-Alk，-N（R11）-SO2-Alk-NR9R10，-N（R11）-SO2-Alk，-N（R11）-Alk-NR5R6，-N（R11）-CO-Alk-NR9R10，-N（R11）-CO-Alk，-N（R11）-CO-CF3，-NH-Alk-HetN，-O-Alk-NR9R10，-O-Alk-CO-NR5R6，-O-Alk-HetN，或R3和R4一起形成5-至6-成员的不饱和杂环，是基本成纤维细胞生长因子的抑制剂。
• 1,2,3-substituted indolizine derivatives, inhibitors of FGFs, method for preparing them and pharmaceutical compositions containing them
  申请人：Sanofi-Aventis

  公开号：US07803811B2

  公开（公告）日：2010-09-28

  The present invention relates to novel 1,2,3-substituted indolizine derivative which are inhibitors of fibroblast growth factors, to methods or preparing such derivatives, to pharmaceutical compositions comprising such derivatives, and to methods of treatment comprising such derivatives.

  本发明涉及一种新型的1,2,3-取代吲哚嗪衍生物，其为成纤维细胞生长因子的抑制剂，以及制备这种衍生物的方法，包括含有这种衍生物的制药组合物，以及包括这种衍生物的治疗方法。
• US7442708B2
  申请人：——

  公开号：US7442708B2

  公开（公告）日：2008-10-28
• US7803811B2
  申请人：——

  公开号：US7803811B2

  公开（公告）日：2010-09-28