7448-86-4Relevant articles and documents
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation
Paucar, Rocío,Martín-Escolano, Rubén,Moreno-Viguri, Elsa,Azqueta,Cirauqui,Marín, Clotilde,Sánchez-Moreno, Manuel,Pérez-Silanes, Silvia
, p. 3902 - 3917 (2019)
The current chemotherapy against Chagas disease is inadequate and insufficient. A series of ten Mannich base-type derivatives have been synthesized to evaluate their in vitro antichagasic activity. After a preliminary screening, compounds 7 and 9 were sub
Rongalite as C1 Synthon and Sulfone Source: A Practical Sulfonylmethylation Based on the Separate-Embedding Strategy
Chen, Xiang-Long,Wu, Chun-Yan,Ma, Jin-Tian,Zhuang, Shi-Yi,Yu, Zhi-Cheng,Wu, Yan-Dong,Wu, An-Xin
supporting information, p. 223 - 227 (2022/01/04)
Rongalite has been used in several challenging synthetic transformations with operationally simple and effective protocols. However, the employment of multiple characteristics of rongalite in synthetic chemistry is comparatively little known. Herein we report a separate-embedding type sulfonylmethylation of sulfoxonium ylides in which rongalite concurrently acted as a sulfone source, C1 synthon, radical initiator, and potential reducing reagent for the first time. Notably, this facile and easy-handling reaction does not require a catalyst or prefunctionalized sulfonylmethylation reagents.
Nickel-Catalyzed C(sp3)-H Functionalization of Benzyl Nitriles: Direct Michael Addition to Terminal Vinyl Ketones
Zhang, Ninghui,Zhang, Chunli,Hu, Xiaoping,Xie, Xin,Liu, Yuanhong
supporting information, p. 6004 - 6009 (2021/07/31)
An efficient nickel(0)-catalyzed addition of benzyl nitriles to terminal vinyl ketones via C(sp3)-H functionalization has been developed. The reaction provides a novel and efficient protocol for the synthesis of α-functionalized benzyl nitriles with a wide range of structural diversity under mild reaction conditions while obviating the use of a strong base. The work might be potentially useful toward the development of an enantioselective variant using chiral nitrogen ligands.
Enantioselective Copper-Catalyzed Electrophilic Sulfenylation of Cyclic Imino Esters
Chen, Zhiwei,Lin, Huaxin,Han, Jian,Fang, Dongmei,Wang, Min,Liao, Jian
supporting information, p. 9146 - 9150 (2021/11/30)
Herein we report an enantioselective sulfenylation of cyclic imino esters with the efficient and versatile sulfenylation reagent S-alkyl 4-methylbenzenesulfonothioates. By utilizing the Cu/tBu-Phosferrox catalytic system, we can assemble diverse S-alkyl groups into the cyclic imino esters under mild conditions in good yields and with excellent enantioselectivities. Remarkably, this method demonstrates a high tolerance of diverse functional groups and proves to be applicable in the late-stage functionalization of pharmaceuticals.