125849-86-7

Upstream product

• 71637-34-8 3-hydroxymethyl-thiophene 
• 58479-61-1 tert-butylchlorodiphenylsilane 
• 117657-67-7 [2-(tert-Butyl-diphenyl-silanyl)-thiophen-3-yl]-methanol 

Downstream Products

• 223254-21-5 1-[4-(tert-butyl-diphenyl-silanyloxymethyl)-thiophen-2-ylmethyl]-4-(2-isopropoxy-phenyl)-piperazine 
• 223254-23-7 {5-[4-(2-isopropoxy-phenyl)-piperazin-1-ylmethyl]-thiophen-3-yl}-methanol 
• 223254-19-1 4-((tert-butyldiphenylsilyloxy)methyl)thiophene-2-carbaldehyde 
• 117657-67-7 [2-(tert-Butyl-diphenyl-silanyl)-thiophen-3-yl]-methanol 

Relevant academic research and scientific papers

QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS

The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

QUINOXALINES AS B RAF INHIBITORS

The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

SUBSTITUTED QUINAZOLONES AS ANTI-CANCER AGENTS

The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

Novel thiophene derivatives for the treatment of benign prostatic hyperplasia

The syntheses and biological activities of a novel series of 2,4- and 2,5-disubstituted thiophenes are reported. These analogues have shown excellent affinity and selectivity against α1-adrenoreceptor subtypes.

Heterocycles useful in the treatment of benign prostatic hyperplasia

This invention relates a to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the α-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.

Regioselective Preparation of 2,4-, 3,4-, and 2,3,4-Substituted Furan Rings. 1. [1,4] O → C and [1,4] C → O Silyl Migrations of Silyl Ethers and Esters Attached to Furan and Thiophene Rings

[1,4] O → C and [1,4] C → O rearrangements are described for a variety of furans and thiophenes. Treatment of 3-((silyloxy)methyl)furans and -thiophenes with n-BuLi in HMPA provided 2-silylated-3-(hydroxymethyl)furans and -thiophenes in good to excellent yields. The reaction was shown by crossover studies to proceed via an intramolecular [1,4] O → C silyl migration. Silyl esters of 3-furoic acids also underwent an intramolecular [1,4] O → C silyl migration to provide 2-silylated-3-furoic acids in moderate to good yield when treated with a mixture of LDA and HMPA. Finally, the above silyl migrations were shown to be reversible. Treatment of 2-silylated-3-(hydroxymethyl)-furans and -thiophenes with NaH in DMF provided 3-((silyloxy)methyl)furans and -thiophenes in excellent yields via a [1,4] C → O silyl migration. The [1,4] C → O silyl migration was also shown to be an intramolecular process by a crossover study.

THE 1,4 CO SILYL MIGRATIONS OF VARIOUS FURAN AND THIOPHENE SYSTEMS

2-Trialkylsilyl-3-hydroxymethyl-furans and -thiophenes undergo a 1,4 CO silyl migration when treated with bases containing either potassium or sodium counterions to produce 3furans and -thiophenes in excellent yields.