- Application of Sulfur Ylides in 1,2-Difunctionalization of Arynes via Insertion into a C-S σ-Bond
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A novel reactivity of sulfur ylides has been demonstrated in a transition-metal-free protocol to access ortho-substituted thioanisole derivatives by insertion of arynes into a C-S σ-bond in moderate to good yields. The reaction involves the formation of C-C and C-S bonds and consecutive breaking of two C-S bonds under operationally mild reaction conditions.
- Ahire, Milind M.,Thoke, Mahesh B.,Mhaske, Santosh B.
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supporting information
p. 848 - 851
(2018/02/10)
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- Redox-Neutral α-Arylation of Alkyl Nitriles with Aryl Sulfoxides: A Rapid Electrophilic Rearrangement
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A facile α-arylation of nitriles has been developed by simply introducing Tf2O and DABCO to the mixture of nitriles and aryl sulfoxides. The transformation consists of two sequential steps: (i) Tf2O-initiated electrophilic assembly a
- Shang, Li,Chang, Yonghui,Luo, Fan,He, Jia-Ni,Huang, Xin,Zhang, Lei,Kong, Lichun,Li, Kaixiao,Peng, Bo
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supporting information
p. 4211 - 4217
(2017/03/27)
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- DI(HETERO)ARYLCYCLOHEXANE DERIVATIVES, THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
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The present invention relates to di(hetero)arylcyclohexane derivatives of the formula (I), in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula (I), their use and pharmaceutical compositions comprising them.
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Page/Page column 94
(2009/01/24)
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- Tetraisoquinoline compounds which have useful pharmaceutical utility
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Tetrahydroisoquinoline compounds of formula I STR1 and pharmaceutically acceptable salts and lipophilic ester thereof have utility as analgesics and in the treatment of psychoses, Parinson''s disease, Lesch-Nyan syndrome, attention deficit disorder or cognitive impairment or in the relief of drug dependence or tardive dyskinesia.
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- REACTION OF 4-CHLORO-1-NITROBENZENE WITH o-SUBSTITUTED PHENYLACETONITRILES; SYNTHESIS OF 8-CHLORO-1-METHYL(AND METHYLTHIOMETHYL)-6-(2-SUBSTITUTED PHENYL)-4H-s-TRIAZOLO-1,4-BENZODIAZEPINES
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Reactions of 4-chloro-1-nitrobenzene with 2-methyl-, 2-methoxy- and 2-(methylthio)phenylacetonitrile in methanolic potassium hydroxide gave mixture from which the excepted 3-aryl-5-chloro-2,1-benzisoxazoles Ia-c were isolated in addition to the 2H-indoles IIIa and IIIc and acridines VIII and IX.The 2,1-benzisoxazoles were reduced to the 2-aminobenzophenones XIIa-c which were transformed via the phthalimidoacetamido compounds XIIIa-c to 5-aryl-7-chloro-1,3-dihydro-1,4-benzodiazepine-2-ones XVa-c.Treatment with phosphorus pentasulfide led to the thiones XVIa-c which reacted in boiling butanol either with acetohydrazide or with (methylthio)acetohydrazide to give the title compounds XVIIa-c and XVIIIa-c.They showed only weak anticonvulsant, incoordinating and central depressant effects.
- Vejdelek, Zdenek,Holubek, Jiri,Ryska, Miroslav,Koruna, Ivan,Svatek, Emil,et.al.
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p. 2545 - 2563
(2007/10/02)
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- SODIUM IODIDE/BORON TRIFLUORIDE ETHERATE: A MILD REAGENT SYSTEM FOR THE CONVERSION OF ALLYLIC AND BENZYLIC ALCOHOLS INTO CORRESPONDING IODIDES AND SULFOXIDES INTO SULFIDES
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A variety of allylic and benzylic alcohols have been converted into the corresponding iodides using NaI/BF3*Et2O.Selective conversion of allylic and benzylic alcohols in preference to primary saturated alcohols has also been demonstrated.Further, the same reagent system has been used to convert sulfoxides into sulfides under mild conditions.
- Vankar, Yashwant D.,Rao, Trinadha C.
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p. 2717 - 2720
(2007/10/02)
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