154355-80-3

Upstream product

• 110-00-9 furan 
• 459-46-1 4-Fluorobenzyl bromide 
• 352-34-1 4-fluoro-1-iodobenzene 
• 98-00-0 (2-furyl)methyl alcohol 
• 403-43-0 4-fluorobenzoyl chloride 

Downstream Products

• 154355-81-4 2-Bromo-5-(4-fluorophenylmethyl)furan 

Relevant academic research and scientific papers

Positional Selectivity in C-H Functionalizations of 2-Benzylfurans with Bimetallic Catalysts

Metal-catalyzed carbon-carbon bond-forming reactions are a mainstay in the synthesis of pharmaceutical agents. A long-standing problem plaguing the field of transition metal catalyzed C-H functionalization chemistry is control of selectivity among inequivalent C-H bonds in organic reactants. Herein we advance an approach to direct site selectivity in the arylation of 2-benzylfurans founded on the idea that modulation of cooperativity in bimetallic catalysts can enable navigation of selectivity. The bimetallic catalysts introduced herein exert a high degree of control, leading to divergent site-selective arylation reactions of both sp2 and sp3 C-H bonds of 2-benzylfurans. It is proposed that the selectivity is governed by cation-π interactions, which can be modulated by choice of base and accompanying additives [MN(SiMe3)2, M = K or Li·12-crown-4].

Intra- and Intermolecular Nickel-Catalyzed Reductive Cross-Electrophile Coupling Reactions of Benzylic Esters with Aryl Halides

Nickel-catalyzed cross-electrophile coupling reactions of benzylic esters and aryl halides have been developed. Both inter- and intramolecular variants proceed under mild reaction conditions. A range of heterocycles and functional groups are tolerated under the reaction conditions. Additionally, the first example of a stereospecific cross-electrophile coupling of a secondary benzylic ester is described. Crossed off: Nickel-catalyzed cross-electrophile coupling reactions of benzylic esters and aryl halides have been developed. Both inter- and intramolecular variants proceed under mild reaction conditions, and a range of heterocycles and functional groups are tolerated. Additionally, the first example of a stereospecific cross-electrophile coupling of a secondary benzylic ester is described.

Substituted arylalkynyl-and heteroarylalkynl-N-hydroxyurea inhibitors of leukotriene biosynthesis

The invention relates to compounds having activity to inhibit lipoxygenase enzyme activity, to pharmaceutical compositions comprising these compounds, and to a medical method of treating. More particularly, this invention concerns certain substituted arylalkynyl- and ((heteroaryl)alkynyl)-N-hydroxy-ureas which inhibit leukotriene biosynthesis, to pharmaceutical compositions of these compounds and to a method of inhibiting leukotriene biosynthesis.

Process for the preparation of methylene compounds and the novel compound 2-(2,4-Dichloro-5-fluorobenzyl)thiophene

Methylene compounds are preferably prepared by reducing an aluminum halide complex of the formula STR1 in which R1 represents a C6 -C10 -aryl radical which is optionally substituted by 1 to 4 C1 -C4 -alkyl radicals, 1 to 4 fluorine, chlorine and/or bromine atoms, one C1 -C8 -alkoxy group and/or one acetoxy group, or represents a heteroaryl radical which is optionally substituted by one C1 -C4 -alkyl radical and/or one fluorine, chlorine or bromine atom and contains 5 to 10 C atoms and one O or S atom and R2 represents a C1 -C12 -alkyl radical which is optionally substituted by 1 to 5 fluorine, chlorine and/or bromine atoms, independently of R1 represents a radical as defined for R1 and, in the case where R1 =a C6 -C10 -aryl radical which is substituted by 1 to 4 fluorine, chlorine and/or bromine atoms, also represents a furyl or thienyl radical, Y represents fluorine, chlorine or bromine, with an amineborane of the formula STR2 in which R3 represents C1 -C4 -alkyl and R4 represents hydrogen or C1 -C4 -alkyl and/or with sodium borohydride and/or with potassium borohydride. 2-(2,4-Dichloro-5-fluorobenzyl)thiophene is obtainable in this way for the first time.

[(SUBSTITUTED) PHENYALKYL]FURYLALKYNYL-AND [SUBSTITUTED)PHENYALKYL]THIENYLALKYNYL-N-HYDROXYUREA INHIBITORS OR LEUKOTRIENE BIOSYNTHESIS

The present invention relates to compounds of the formula and the pharmaceutically acceptable salts thereof wherein Z is selected from optionally substituted phenyl, furyl, thienyl or thiazolyl; which inhibits leukotriene biosynthesis and is useful in the treatment of inflammatory disease states; also disclosed are leukotriene biosynthesis inhibiting compositions and a method for inhibiting 5-lipoxygenase activity and leukotriene biosynthesis