229640-29-3

Upstream product

• 267659-62-1 methanesulfonic acid 4-bromo-3-methylphenyl ester 
• 34241-39-9 azobisisobutyronitrile 
• 14472-14-1 4-bromo-3-methylphenol 

Downstream Products

• 1471471-41-6 methanesulfonic Acid 4-Bromo-3-(3-tert-butoxycarbonylamino-2-oxopyrrolidin-1-ylmethyl)phenyl Ester 
• 254108-64-0 4-[1-(4-Cyano-3-fluorobenzyl)-5-imidazolylmethyl]-1-[2-bromo-5-((methanesulfonyl)-oxy)benzyl]-2-piperazinone 
• 676319-77-0 methanesulfonic acid 4-bromo-3-(2-oxo-piperazin-1-ylmethyl)-phenyl ester 
• 267659-63-2 1-[2-Bromo-5-((methanesulfonyl)oxy)benzyl]-4-tert-butoxycarbonyl-2-piperazinone 
• 229640-26-0 methanesulfonic acid 4-bromo-3-(2-oxo-pyrrolidin-1-ylmethyl)-phenyl ester 

Relevant academic research and scientific papers

Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I

A series of macrocyclic piperazinone compounds with dual farnesyltransferase/geranylgeranyltransferase-I inhibitory activity was prepared. These compounds were found to be potent inhibitors of protein prenylation in cell culture. A hypothesis for the binding mode of compound 3o in FPTase is proposed.

INHIBITORS OF PRENYL-PROTEIN TRANSFERASE

The present invention is directed to peptidomimetic piperazine-containing macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras

Inhibitors of prenyl-protein transferase

The present invention is directed to macrocyclic compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemothera-peutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Inhibitors of prenyl-protein transferase

The present invention is directed to peptidomimetic macrocyclic compounds of the formula A: wherein W is a heterocycle, V is a heterocycle or aryl moiety and Z1is a suitably substituted aryl or heterocycle moiety. The instant compounds inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Arylmethanesulfonates are convenient latent phenols in the nucleophilic aromatic substitution reaction

The methanesulfonyl protecting group for a phenol is conveniently unmasked under the conditions of the S(N)Ar reaction with an activated aryl halide, producing diarylether products directly. The method is advantageous when the preparation of a phenol substrate requires O-protection, since the selection of the robust methanesulfonate as a latent phenol obviates a deprotection step prior to the S(N)Ar reaction.