A concise synthesis of a novel insulin-like growth factor I receptor (IGF-IR) inhibitor

Slade J; Bajwa J; Liu H; Parker D; Vivelo J; Chen GP; Calienni J; Villhauer E; Prasad K; Repic O

首页> 外文期刊>Organic process research & development >A concise synthesis of a novel insulin-like growth factor I receptor (IGF-IR) inhibitor

【24h】

A concise synthesis of a novel insulin-like growth factor I receptor (IGF-IR) inhibitor

机译：新型胰岛素样生长因子I受体（IGF-IR）抑制剂的简明合成

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

An efficient synthesis of a potent insulin-like growth factor I receptor (IGF-IR) hihibitor AEW541 (1) is described. The key step in the synthesis is the cis-selective reductive amination of cyclobutanone, which sets up the desired 1,3-stereochemistry of the cyclobutane ring. The amino group thus generated is used as a handle to build the pyrrolopyrimidine ring. The final step resulting in 1 is accomplished by alkylation of in situ generated mesylate with azetidine.

机译：描述了有效的胰岛素样生长因子I受体（IGF-1R）抑制剂AEW541（1）的有效合成。合成中的关键步骤是环丁酮的顺式-选择性还原胺化，可建立所需的环丁烷环的1,3-立体化学。由此产生的氨基被用作构建吡咯并嘧啶环的手柄。通过用氮杂环丁烷原位产生的甲磺酸盐的烷基化来完成产生1的最后步骤。

著录项

来源
《Organic process research & development》 |2007年第5期|共11页
作者
Slade J; Bajwa J; Liu H; Parker D; Vivelo J; Chen GP; Calienni J; Villhauer E; Prasad K; Repic O;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类有机化学;
关键词

相似文献

外文文献
中文文献
专利

1. A concise synthesis of a novel insulin-like growth factor I receptor (IGF-IR) inhibitor [J] . Slade J, Bajwa J, Liu H, Organic process research & development . 2007,第5期

机译：新型胰岛素样生长因子I受体（IGF-IR）抑制剂的简明合成
2. Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases. [J] . Hubbard RD, Bamaung NY, Fidanze SD, Bioorganic and Medicinal Chemistry Letters . 2009,第6期

机译：胰岛素样生长因子受体（IGF-IR）的多靶向抑制剂的研制和表皮生长因子受体酪氨酸激酶的成员。
3. Inhibition of insulin-like growth factor-I receptor (IGF-IR) using NVP-AEW541, a small molecule kinase inhibitor, reduces orthotopic pancreatic cancer growth and angiogenesis. [J] . Moser C, Schachtschneider P, Lang SA, European journal of cancer: official journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR) . 2008,第11期

机译：使用小分子激酶抑制剂NVP-AEW541抑制胰岛素样生长因子-I受体（IGF-IR），可减少原位胰腺癌的生长和血管生成。
4. NOVEL APPROACHES WITH HEPATITIS B CORE CARRIER IN THE GROWTH CONTROL OF HepG2 BY BLOCKADE OF INSULIN-LIKE GROWTH FACTOR-Ⅰ RECEPTOR (IGF-IR) [C] . Jing Kong, Zhengyu Diao, Xiaozhao Deng, 第四届国际后基因组生命科学技术学术论坛 . 2006

机译：胰岛素样生长因子-Ⅰ受体（IGF-IR）阻滞HepG2生长控制的新型肝癌载体的新方法
5. Suppressor of cytokine signaling-2 (SOCS2) and epidermal growth factor (EGF) modulate insulin-like growth factor-I receptor (IGF-IR) signaling in intestinal cancer. [D] . Newton, Victoria A. 2010

机译：细胞因子信号传导抑制因子2（SOCS2）和表皮生长因子（EGF）的抑制因子调节肠癌中胰岛素样生长因子-I受体（IGF-IR）的信号传导。
6. Dopamine by Acting through Its D2 Receptor Inhibits Insulin-Like Growth Factor-I (IGF-I)-Induced Gastric Cancer Cell Proliferation via Up-Regulation of Krüppel-Like Factor 4 through Down-Regulation of IGF-IR and AKT Phosphorylation [O] . Subhalakshmi Ganguly, Biswarup Basu, Saurav Shome, 2010

机译：多巴胺通过其D2受体发挥作用通过下调IGF-IR和AKT磷酸化而上调类似Krüppel因子4抑制胰岛素样生长因子-I（IGF-I）诱导的胃癌细胞的增殖。
7. Implication of RICTOR in the mTOR inhibitor-mediated induction of insulin-like growth factor-I receptor (IGF-IR) and human epidermal growth factor receptor-2 (Her2) expression in gastrointestinal cancer cells [O] . Lang Sven A., Hackl Christina, Moser Christian, 2010

机译：RICTOR在胃肠癌细胞中mTOR抑制剂介导的胰岛素样生长因子I受体（IGF-IR）和人表皮生长因子受体2（Her2）表达的诱导中的意义
8. Therapy of Prostate Cancer Using a Human Antibody Targeting the Type 1 Insulin-Like Growth Factor Receptor (IGF-IR) [R] . Plymate, S. R. 2009

机译：使用针对1型胰岛素样生长因子受体（IGF-IR）的人抗体治疗前列腺癌

A concise synthesis of a novel insulin-like growth factor I receptor (IGF-IR) inhibitor

摘要

著录项

相似文献

相关主题

期刊订阅