CAS: 183204-72-0; 5-Chloro-6-((2-Iminopyrrolidin-1-yl)Methyl)Pyrimidine-2,4(1H,3H)-Dione Hydrochloride

6-甲基尿嘧啶置于sodium Tetrahydroborate,氯化亚砜,Sodium Ethanolate,溶剂黄146,Copper(II) Oxide体系中,用 四氢呋喃,二氯甲烷,水,N,N-二甲基甲酰胺 用作溶剂,20.0~110.0 °C,101.33 Kpa 条件下,反应 27.33H,反应生成(9Ci)-5-氯-6-[(2-亚氨基-1-吡咯烷)甲基]-2,4(1H,3H)-嘧啶二酮盐酸盐
参考文献:一种盐酸替匹嘧啶及其中间体6-氯甲基尿嘧啶的合成方法
标题:一种盐酸替匹嘧啶及其中间体6-氯甲基尿嘧啶的合成方法
摘要:本发明提供了一种6‑氯甲基尿嘧啶的合成方法,包括:将6‑甲基尿嘧啶与氧化铜在溶剂中进行氧化反应,得到6‑甲酰基尿嘧啶;还原6‑甲酰基尿嘧啶,得到6‑羟甲基尿嘧啶;将6‑羟甲基尿嘧啶经氯代反应,得到6‑氯甲基尿嘧啶,所得6‑氯甲基尿嘧啶的纯度＞99.0%.本发明优化了6‑氯甲基尿嘧啶的合成方法,以低毒性的金属氧化剂代替了二氧化硒实现6‑甲基尿嘧啶的氧化工艺,增加环境友好性,同时提高了6‑氯甲基尿嘧啶的收率及纯度.本发明还提供了一种盐酸替匹嘧啶的合成方法,采用上述工艺所得6‑氯甲基尿嘧啶为中间体,经氯代,缩合,成盐三步反应直接制得盐酸替匹嘧啶,所得原料药无需任何纯化过程,纯度高于99.0%.

专利信息

专利号:US-2022118094-A1
优先权日:2019-02-21
标题:Synthesis of biomimetic cell wall structure
发明人：WANG YONG; SHI PENG
权利人:PENN STATE RES FOUND
摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

专利号:US-2023391824-A1
优先权日:2021-02-08
标题:Rationale, design, synthesis and validation of a small molecule anticancer agent
发明人：JAIN MOHIT; NARENDRAN ARUMUGAVADIVEL
权利人:NARENDRAN ARUMUGAVADIVEL
摘要:LIN28 is an RNA binding protein that binds and inhibits the expression and maturation of Iet7 microRNA that carries key tumor suppressor functions. Thus, LIN28 is a feasible and effective molecular target for directed inhibition with the potential to provide therapeutic benefit to a diverse group of aggressive malignancies. The present disclosure relates generally to the Rationale, Design, Synthesis and Validation of a Novel Small Molecule Inhibitor of LIN28, coined Compound of formula (I), for the Treatment of Adult and Pediatric Malignancies. In addition, indications of this agent to block cancer metastasis, inhibit cancer stem cells to prevent relapse, and to synergize with immunotherapy, chemotherapy and radiotherapy are also been described.

专利号:EP-4288444-A1
优先权日:2021-02-08
标题:Rationale, design, synthesis and validation of a small molecule anticancer agent

专利号:WO-2022165606-A1
优先权日:2021-02-08
标 题:Rationale, design, synthesis and validation of a small molecule anticancer agent

专利号:CA-3207354-A1
优先权日:2021-02-08
标题:Rationale, design, synthesis and validation of a small molecule anticancer agent