Monomethylierte 3-Thiacyclopentylsulfaminsäuren und ihre Süßstoffeigenschaften
作者:B. Unterhalt、L. Kerckhoff、M. Möllers
DOI:10.3797/scipharm.aut-00-09
日期:——
Methyl-3-thiacyclopentanarnines 4a-c were reacted to their sulfamic acid sodiurn salts 5a-c, and their structures determined.Only sodium 4-methyl-3-thiacyclopentylsulfamate (5b) is sweet. The oxa analogues 8a-b however are tasteless.
An Old Story in the Parallel Synthesis World: An Approach to Hydantoin Libraries
作者:Andrey V. Bogolubsky、Yurii S. Moroz、Olena Savych、Sergey Pipko、Angelika Konovets、Maxim O. Platonov、Oleksandr V. Vasylchenko、Vasyl V. Hurmach、Oleksandr O. Grygorenko
DOI:10.1021/acscombsci.7b00163
日期:2018.1.8
An approach to the parallel synthesis of hydantoin libraries by reaction of in situ generated 2,2,2-trifluoroethylcarbamates and α-amino esters was developed. To demonstrate utility of the method, a library of 1158 hydantoins designed according to the lead-likeness criteria (MW 200–350, cLogP 1–3) was prepared. The success rate of the method was analyzed as a function of physicochemical parameters