135822-87-6Relevant articles and documents
Direct Mannich-Type Reactions Promoted by Frustrated Lewis Acid/Br?nsted Base Catalysts
Chan, Jessica Z.,Yao, Wenzhi,Hastings, Brian T.,Lok, Charles K.,Wasa, Masayuki
supporting information, p. 13877 - 13881 (2016/10/26)
Direct Mannich-type reactions that afford both α- and β-amino esters by the reaction of a broad range of carbonyl compounds and aldimines are disclosed. The transformation is promoted by a sterically frustrated Lewis acid/Br?nsted base pair, which is prop
Triarylmethyl chlorides as novel, efficient, and mild organic catalysts for the synthesis of N-sulfonyl imines under neutral conditions
Khalafi-Nezhad, Ali,Parhami, Abolfath,Zare, Abdolkarim,Shirazi, Amir Nasrolahi,Zare, Ahmad Reza Moosavi,Hassanimejad, Alireza
, p. 456 - 461 (2008/09/20)
A highly efficient procedure for the preparation of N-sulfonyl imines via condensation of sulfonamides with aldehydes as well as ketones in the presence of triarylmethyl chlorides as metal-free organo-catalysts at 40 °C is described. The advantages of thi
Small-molecule inhibitors of protein geranylgeranyltransferase type I
Castellano, Sabrina,Fiji, Hannah D. G.,Kinderman, Sape S.,Watanabe, Masaru,De Leon, Pablo,Tamanoi, Fuyuhiko,Kwon, Ohyun
, p. 5843 - 5845 (2008/03/14)
Small molecules that inhibit the geranylgeranylation of K-Ras4B and RhoA by protein geranylgeranyltransferase type I (GGTase-I) were identified from chemical genetic screens of heterocycles synthesized through phosphine catalysis of allenes. To further improve the efficacy of the GGTase-I inhibitors (GGTIs), 4288 related compounds bearing core dihydropyrrole/pyrrolidine and tetrahydropyridine/piperidine scaffolds were synthesized on SynPhase lanterns in a split-pool manner through phosphine-catalyzed [3 + 2] and [4 + 2] annulations of resin-bound allenoates. Testing of the 4288 analogues resulted in several GGTIs exhibiting submicromolar IC50 values. Because proteins such as Ras and Rho GTPases are implicated in oncogenesis and metastasis, these GGTIs might ultimately lead to the development of novel antitumor therapeutics. Copyright