29604-25-9Relevant academic research and scientific papers
Decarboxylative etherification of aromatic carboxylic acids
Bhadra, Sukalyan,Dzik, Wojciech I.,Goossen, Lukas J.
, p. 9938 - 9941 (2012/08/08)
Decarboxylative Chan-Evans-Lam-type couplings are presented as a new strategy for the regiospecific construction of diaryl and alkyl aryl ethers starting from easily available aromatic carboxylic acids. They allow converting various aromatic carboxylate salts into the corresponding aryl ethers by reaction with alkyl orthosilicates or aryl borates, under aerobic conditions in the presence of silver carbonate as the decarboxylation catalyst and copper acetate as the cross-coupling catalyst.
Ortho-selectivity in SNAr substitutions of 2,4-dihaloaromatic compounds. Reactions with anionic nucleophiles
Wendt, Michael D.,Kunzer, Aaron R.
scheme or table, p. 3041 - 3044 (2010/07/18)
The nucleophilic addition of organic anions to aromatic compounds with halogens positioned both ortho and para to activating groups was studied in a variety of solvents. Substrates showed strong preferences for ortho substitution in most cases. Evidence is presented for activating group-dependent coordination, which contributes to very high ortho-selectivity in nonpolar solvents. This also drives the overall reaction rate in these solvents, and is of close to the same magnitude of rate increase derived from polar solvents. para-Products are maximized by using crown ethers in protic solvents. Solvent effects overall are very different from corresponding reactions with amine nucleophiles due primarily to the different charges present in the transition states, and to solvation of the nucleophile.
Compounds useful in therapy
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Page/Page column 53, (2010/02/12)
Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: X represents —[CH2]a—R or —[CH2]a—O—[CH2]b—R; a represents a number selected from 0 to 6; b represents a number selected from 0 to 6; R represents H, CF3 or Het; Het represents an optionally substituted 5- or 6-membered saturated, partially saturated or aromatic heterocyclic ring; Y represents one or more substituents independently selected from —[O]c—[CH2]d—R1, which may be the same or different at each occurrence; c at each occurrence independently represents a number selected from 0 or 1; d at each occurrence independently represents a number selected from 0 to 6; R1 at each occurrence independently represents H, halo, CF3, CN or Het1; Het1 at each occurrence independently represents a 5- or 6-membered unsaturated heterocyclic ring; V represents a direct link or —O—; Ring A represents an optionally substituted 5- to 7-membered saturated heterocyclic ring, or a phenylene group; Q represents a direct link or —N(R2)—; R2 represents hydrogen or C1-6 alkyl; Z represents —[O]e—[CH2]f—R3, a phenyl ring (optionally fused to a benzene ring or Het2, and the group as a whole being optionally substituted), or Het3 (optionally fused to an benzene ring or Het4, and the group as a whole being optionally substituted); R3 represents C1-6 alkyl (optionally substituted), C3-6 cycloalkyl, C3-6 cycloalkenyl, phenyl (optionally substituted), Het5 or NR4R5; e represents a number selected from 0 or 1; f represents a number selected from 0 to 6; Het2 and Het5 independently represent optionally substituted 5- or 6-membered saturated, partially saturated or aromatic heterocyclic rings; Het3 represents an optionally substituted 4 to 6-membered saturated, partially saturated or aromatic heterocyclic ring; Het4 represents an optionally substituted 6-membered aromatic heterocyclic ring; R4 and R5 independently represent optionally substituted C1-6 alkyl, C1-6 alkyloxy, C3-8 cycloalkyl (optionally fused to C3-8 cycloalkyl), Het6, or hydrogen; Het6 represents an optionally substituted 5- or 6-membered saturated, partially saturated or aromatic heterocyclic ring; are useful for treating a disorder for which a V1a antagonist is indicated.
