磺酰氯不仅在保护基团化学中发挥着至关重要的作用,而且还是磺酰胺合成中的重要起始原料,而磺酰胺是药物发现化学中急需的基序。尽管磺酰氯很重要,但不同合成方法的数量有限,其中大多数依赖于硫醇前体的传统氧化氯化化学。在本报告中,我们公开了一种在 HCl 和 Cu 催化剂存在下,由原料苯胺和 DABSO(用作稳定的 SO 2替代物)进行的新型桑德迈尔型磺酰氯合成方法。该方法适用于多种苯胺,并允许在水性后处理后分离磺酰氯,或在桑德迈尔反应完成后通过简单添加胺将磺酰氯直接转化为磺酰胺。该方法的可扩展性在 20 g 规模上得到了证明,并且以 80% 的产率和优异的纯度分离出相应的杂环磺酰氯。
Compounds and methods for inhibiting growth of a protozoan parasite. Methods of treating a protozoan parasite infection in a subject by administering a therapeutically effective amount of a compound as disclosed herein. The compounds and methods can be used to inhibit growth of protozoan parasites such as
Trypanosoma brucei, Trypanosoma cruzi, Leishmania
spp., and
Plasmodium
spp.
[EN] 4-OXO-3,4-DIHYDROQUINAZOLINE COMPOUNDS AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION<br/>[FR] COMPOSÉS DE 4-OXO-3,4-DIHYDROQUINAZOLINE UTILISÉS EN TANT QU'INHIBITEURS DE LA RÉPLICATION DU VIRUS DE L'IMMUNODÉFICIENCE HUMAINE
申请人:VIIV HEALTHCARE UK NO 5 LTD
公开号:WO2019198024A1
公开(公告)日:2019-10-17
Compounds of Formula (I), including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth: Formula (I):
COMPOUNDS FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISEASE
申请人:SHY Therapeutics LLC
公开号:US20170174699A1
公开(公告)日:2017-06-22
Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease.
The present invention provides a compound of Formula (I)
as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.