- Preparation method of fostamatinib key intermediate and intermediate thereof and method for preparing fostamatinib with intermediate
-
The invention discloses a preparation method of a fostamatinib key intermediate and an intermediate thereof and a method for preparing fostamatinib with the intermediate. The preparation method of thefostamatinib key intermediate comprises the following steps: carrying out a nucleophilic substitution reaction on a compound (2) and a compound (3) so as to obtain a fostamatinib key intermediate compound (4), and carrying out reduction cyclization on the compound (4), thereby obtaining a fostamatinib key intermediate compound (1), wherein the reaction formula is as shown in the specification. The preparation method disclosed by the invention is easy in raw material and reagent obtaining, low in price, low in cost and easy in industrialization and has the advantages of being high in synthesisyield, good in product purity, and the like.
- -
-
Paragraph 0053-0064
(2019/07/04)
-
- Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer
-
Prostate cancer is a commonly diagnosed cancer and a leading cause of cancer-related deaths. The bromodomain and extra terminal domain (BET) family proteins have emerged as potential therapeutic targets for the treatment of castration-resistant prostate cancer. A series of 2,2-dimethyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives were designed and synthesized as selective bromodomain containing protein 4 (BRD4) inhibitors. The compounds potently inhibit BRD4(1) with nanomolar IC50 values and exhibit high selectivity over most non-BET subfamily members. One of the representative compounds 36 (Y08060) effectively suppresses cell growth, colony formation, and expression of androgen receptor (AR), AR regulated genes, and MYC in prostate cancer cell lines. In in vivo studies, 36 demonstrates a good PK profile with high oral bioavailability (61.54%) and is a promising lead compound for further prostate cancer drug development.
- Xiang, Qiuping,Zhang, Yan,Li, Jiaguo,Xue, Xiaoqian,Wang, Chao,Song, Ming,Zhang, Cheng,Wang, Rui,Li, Chenchang,Wu, Chun,Zhou, Yulai,Yang, Xiaohong,Li, Guohui,Ding, Ke,Xu, Yong
-
p. 262 - 267
(2018/03/21)
-
- ALKYLIDINE SUBSTITUTED HETEROCYCLYL DERIVATIVES AS ANTI-BACTERIAL AGENTS
-
The present invention relates to alkylidine substituted heterocyclyl derivatives of formula (1) which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors; I in which P, Q, Ri, R2, R3 and "n" have the same meanings given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FABI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
- -
-
Page/Page column 22
(2015/06/03)
-
- [Omim][BF4], a green and recyclable ionic liquid medium for the one-pot chemoselective synthesis of benzoxazinones
-
An efficient procedure for the one-pot chemoselective synthesis of 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives from their corresponding o-aminophenols is developed using DBU in the ionic liquid [omim][BF4]. Upon completion of the reaction and separation of the product, the ionic liquid is recovered and successfully reused over nine recycles without any noticeable loss of performance.
- Sharifi, Ali,Barazandeh, Mehdi,Saeed Abaee,Mirzaei, Mojtaba
-
experimental part
p. 1852 - 1855
(2010/09/07)
-
