Substituted 2-arylcarbonyloxymethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
2-Heterocyclyloxymethyl and 2-heterocyclylthiomethyL-1,2,5-thiadiazolidin-3-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
GRAPHICAL ABSTRACT ABSTRACT An efficient protocol was developed for the synthesis of N-sulfonylimines under environment friendly conditions. Ultrasonic energy was employed to obtain the desired products in excellent yields with high purity under solvent- and catalyst-free conditions. The synthesis of new N-sulfonylimines was accomplished from various N-sulfonamides and benzaldehyde. The structures
图形摘要 摘要 开发了一种在环境友好条件下合成 N-磺酰亚胺的有效方案。在无溶剂和无催化剂的条件下,采用超声波能以高产率和高纯度获得所需产品。新的N-磺酰亚胺的合成是由各种N-磺酰胺和苯甲醛完成的。合成化合物的结构通过元素分析以及 1H、13C NMR 光谱数据、IR 和 MS 确认。
[EN] 2-HETEROCYCLYLOXY AND THIOMETHYL-1,2,5-THIADIAZOLIDIN-3-ONE 1,1-DIOXIDES AND COMPOSITIONS AND METHOD OF USE THEREOF<br/>[FR] 1,1-DIOXYDES DE 2-HETEROCYCLYLOXY ET THIOMETHYL-1,2,5-THIADIAZOLIDIN-3-ONE, COMPOSITIONS ET PROCEDE D'UTILISATION
申请人:SANOFI WINTHROP, INC.
公开号:WO1996016649A1
公开(公告)日:1996-06-06
(EN) 2-Heterocyclyloxy and thiomethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.(FR) 1,1-dioxydes de 2-hétérocyclyloxy et thiométhyl-1,2,5-thiadriazolidin-3-one, compositions pharmaceutiques contenant ces composés et procédés d'utilisation de ces composés pour le traitement des maladies dégénératives.
A green and simple approach for the N-Boc protection on structurally diverse amines under ultrasound irradiation is described. Selective N-Boc protection was achieved in excellent isolated yield in a short reaction time at room temperature. Mild conditions, inexpensive and an easily available reagent, and absence of any auxiliary substances are the main advantages of this procedure.