- Pd-Catalyzed Regioselective Branched Hydrocarboxylation of Terminal Olefins with Formic Acid
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A regioselective Pd-catalyzed hydrocarboxylation of terminal olefins with HCOOH is described. A wide variety of branched carboxylic acids can readily be obtained with high regioselectivities under mild reaction conditions. The reaction is operationally simple and requires no handling of toxic CO. The ligand and LiCl are important factors for reaction reactivity and selectivity.
- Chu, Jianxiao,Guo, Jianqiong,Ren, Wenlong,Shi, Yian,Shi, Yuan,Wang, Mingzhou,Zhou, Jintao
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supporting information
p. 886 - 891
(2022/02/07)
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- Synthetic method of acid compound
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The invention belongs to the field of organic synthesis, and particularly relates to a synthetic method of an acid compound. An acid anhydride compound and an alkyl bromide or a functionalized alkyl bromide are subjected to a cross-electrophilic coupling reaction to synthesize an acid compound, so that the application of the alkyl bromide in the cross-electrophilic coupling reaction is expanded, and a novel non-traditional method for chemically and selectively constructing a carbon-carbon bond through a decarburization process is provided. The synthesis method is simple, economic, green and environment-friendly, and has wider applicability or is suitable for large-scale production.
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Paragraph 0028-0032; 0058
(2020/08/25)
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- Cp2TiCl2-Catalyzed Regioselective Hydrocarboxylation of Alkenes with CO2
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Cp2TiCl2-catalyzed regioselective hydrocarboxylation of alkenes with CO2 to give carboxylic acids in high yields has been developed in the presence of iPrMgCl. The reaction proceeds with a wide range of alkenes under mild conditions. Styrene and its derivatives can transform to α-aryl carboxylic acids, and aliphatic alkenes can transform to form alkanoic acids.
- Shao, Peng,Wang, Sheng,Chen, Chao,Xi, Chanjuan
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supporting information
p. 2050 - 2053
(2016/06/01)
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- Reductive cleavage of 2,2,2-trichloroethyl esters with sodium telluride
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Carboxylic acids are regenerated from their 2,2,2,-trichloroethyl esters by treatment with sodium telluride in dimethylformamide in smooth conditions and with good yields. The reaction conditions are compatible with other functional and protective groups such as methyl ester, acetate or tert- butyldimethylsilyl ethers.
- Blay, Gonzalo,Cardona, Luz,Garcia, Begona,Garcia, Cristina L.,Pedro, Jose R.
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p. 1405 - 1414
(2007/10/03)
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- 2-Substituted histamines with G-protein-stimulatory activity
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The cationic-amphiphilic 2-substituted histamines, 2-(2-chlorophenyl)histamine (2-ethanamine) and 2-(2-cyclohexylethyl)histamine, activate pertussis toxin-sensitive guanine nucleotide-binding proteins (G-proteins) of the Gi-subfamily by a receptor-independent mechanism.We studied structure-activity relationships of 2-substituted histamine derivatives for this G-protein activation using six known and 12 newly synthesized compounds.Elongation of the alkyl chain between imidazole and the ring system enhanced the potency and efficiency of substances in activating high-affinity GTP hydrolysis, ie the enzymatic activity of G-protein α subunits, in membranes of HL-60 leukemic cells.Cyclopentyl-, cyclohexyl- and norbornyl-substituted histamines were more effective and potent than phenyl-substituted histamines in mediating G-protein activation in HL-60 membranes and in activating reconstituted bovine brain Gi/Go-proteins.Our data show that the chain length and the type of ring system are important determinants for receptor-independent G-protein activation by 2-substituted histamines.With respect to histamine H1-receptors, most of the substances studied displayed weak antagonistic activity.
- Detert, H.,Hagelueken, A.,Seifert, R.,Schunack, W.
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p. 271 - 276
(2007/10/02)
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- Nickelalactone als Synthesebausteine: Sonochemische und Bimetallsktivierung der Kreuzkopplungsreaction mit Alkyl-halogeniden
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Nickelalactones with five- and six-membered chelate ring structures can be synthesized in a simple one-pot reaction, starting from Ni(acac)2, bipy, Et3Al and cyclic anhydrides.In the presence of MnI2 and by activation with ultrasound they react selectively with alkyl iodides in cross coupling reactions.The reason for the activating effect of MnI2 is the formation of bimetallic complexes.Many reactive functional groups (e.g.COOR, CHO, CN) can be tolerated.Therefore the cross coupling reaction is of preparative value in the synthesis of functionalized carboxylic acids.
- Fischer, Reinald,Walther, Dirk,Braeunlich, Gabriele,Undeutsch, Bernd,Ludwig, Werner
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p. 395 - 407
(2007/10/02)
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- 5,6-epoxy-7-oxabicycloheptane substituted diamide prostaglandin analogs
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5,6-Epoxy-7-oxabicycloheptane substituted diamide prostaglandin analogs are provided having the structural formula STR1 wherein A is --CH=CH-- or --CH2 --CH2 --; n is 1 to 5; R is CO2 H, CO2 alkyl, CO2 alkali metal, CO2 polyhydroxyamine salt or STR2 q is 1 to 12; and R1 is H, lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, STR3 (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
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- 7-thiabicycloheptane substituted diamide and its congener prostaglandin analogs
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7-Thiabicycloheptane substituted diamide and congener prostaglandin analogs are provided having the structural formula STR1 wherein m is 1 to 4; A is --CH=CH-- or --CH2 --CH2 --; n is 1 to 5; R is CO2 H, CO2 alkyl, CO2 alkali metal, CO2 polyhydroxyamine salt, --CH2 OH, STR2 wherein R3 and R4 are the same or different and are H, lower alkyl, hydroxy, lower alkoxy or aryl, at least one of R3 and R4 being other than hydroxy and lower alkoxy; p is 1 to 4; Z is STR3 q is 1 to 12; R1 is H or lower alkyl; and R3 is H, lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, STR4 (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
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- 7-OXABICYCLOHEPTANE SUBSTITUTED DIAMIDE AND ITS CONGENER PROSTAGLANDIN ANALOGS USEFUL IN THE TREATMENT OF THROMBOTIC DISEASE
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7-Oxabicycloheptane substituted amide prostaglandin analogs are provided having the structural formula STR1 wherein m is 0 to 4; A is--CH=CH--or--CH 2--CH 2--; n is 1 to 5; Q is--CH=CH--,--CH 2--, STR2 or a single bond; R is CO 2 H, CO 2 alkyl, CO 2 alkali metal, CO 2 polyhydroxyamine salt,--CH 2 OH, STR3 wherein R. sup.4 and R 5 are the same or different and are H, lower alkyl, hydroxy, lower alkoxy or aryl, at least one of R 4 and R 5 being other than hydroxy and lower alkoxy; p is 1 to 4; R. sup.1 is H or lower alkyl; q is 1 to 12; R 2 is H or lower alkyl; and R 3 is H, lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, STR4 (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
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