270929-33-4

Upstream product

• 3764-01-0 2,4,6-trichloropyrimidine 
• 42116-44-9 N-tert-butoxycarbonylbenzylamine 

Downstream Products

• 90042-88-9 4-benzilamino-2,6-tricloropirimidina 
• 1067679-65-5 benzyl-(6-chloro-2-(3-methyl-butyl)-pyrimidin-4-yl)-carbamic acid tert-butyl ester 
• 1067679-35-9 benzyl-(2-chloro-6-(3-methyl-butyl)-pyrimidin-4-yl)-carbamic acid tert-butyl ester 
• 1067679-38-2 benzyl-(2-chloro-6-(2-naphthalen-1-yl-ethyl)-pyrimidin-4-yl)-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

Regioselective 4-amino-de-chlorination of trichloro- and dichloro-pyrimidines with N-sodium carbamates

4-N-Alkoxycarbonylamino-2,6-dichloro- and -2-chloro-pyrimidines have been synthesized in good to excellent regioselectivity and yields from N-sodium carbamates and, respectively, 2,4,6-trichloropyrimidine and 2,4-dichloropyrimidine, in DMF, rt, 15-30 min. The reaction is effective also with 4,6-dichloropyrimidine, producing 4-N-alkoxycarbonylamino-6-chloropyrimidines in good yields. Some conformational features of 4-N-alkoxycarbonylamino-2,6-dichloro-pyrimidines have been investigated by X-ray diffraction and 1H NMR spectroscopy.

Blocking estrogen signaling after the hormone: Pyrimidine-core inhibitors of estrogen receptor-coactivator binding

As an alternative approach to blocking estrogen action, we have developed small molecules that directly disrupt the key estrogen receptor (ER)/coactivator interaction necessary for gene activation. The more direct, protein-protein nature of this disruption might be effective even in hormone-refractory breast cancer. We have synthesized a pyrimidine-core library of moderate size, members of which act as α-helix mimics to block the ERα/coactivator interaction. Structure-activity relationships have been explored with various C-, N-, O-, and S-substituents on the pyrimidine core. Time-resolved fluorescence resonance energy transfer and cell-based reporter gene assays show that the most active members inhibit the ERα/steroid receptor coactivator interaction with Ki's in the low micromolar range. Through these studies, we have obtained a refined pharmacophore model for activity in this pyrimidine series. Furthermore, the favorable activities of several of these compounds support the feasibility that this coactivator binding inhibition mechanism for blocking estrogen action might provide a potential alternative approach to endocrine therapy.

Efficient and regioselective 4-amino-de-chlorination of 2,4,6- trichloropyrimidine with N-sodium carbamates

4-N-Alkoxycarbonyl-2,6-dichloropyrimidines have been synthesized with good to excellent regioselectivity and yields from 2,4,6-trichloropyrimidine and N-sodium carbamates in DMF, at room temperature, in 15-30 minutes. (C) 2000 Elsevier Science Ltd.