- Preparation and characterization of poly[2,3-dimethyl-1-(4-thien-3-ylbenzyl)-1H-imidazol-3-ium] bis((trifluoromethyl)sulfonyl)imide
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A new 3-fluorophenylthiophene derivative bearing a cationic imidazolium group in the para position of the phenyl ring was synthesized by a multistep procedure which involves, in a key step, the reaction of 3-[4-(bromomethyl)phenyl]thiophene with 1,2-dimet
- Naudin, Eric,Ho, Hoang Anh,Bonin, Marc-Andre,Breau, Livain,Belanger, Daniel
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- Synthesis of novel alkyl- and aryl sulfides and thiols as precursors for self-assembled monolayers on gold
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A series of 4-alkyl-1-bromosulfanylbenzenes having S-methyl 2, S-t-butyl 3, S-trityl 4, S-benzyl S, and S-silylethoxymethyl 6 substituents were prepared and evaluated for their ability to form a monolayer consisting of an S-aryl adsorbate on Au (111) surf
- Touaibia, Mohamed,Desjardins, Marc-Andre,Provencal, Alexandre,Audet, Daniel,Medard, Christelle,Morin, Mario,Breau, Livain
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p. 2283 - 2288
(2007/10/03)
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- Endothelin receptor antagonists
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The present invention provides novel compounds represented by the general formula I: STR1 wherein R 1 is a straight or branched lower alkyl, a cycloalkyl-lower alkyl, an aryl-lower alkyl, a cycloalkyl, an aryl an aryl-cycloalkyl, lower alkoxy, an aryloxy, or a heteroaryl;R 2 is hydrogen, a straight or branched lower alkyl, a cycloalkyl, or a cycloalkyl-lower alkyl;R 3 and R 3 '' are each the same or different and each is hydrogen atom, a straight or branched lower alkyl, a cycloalkyl, an aryl-lower alkyl, an aryl, or a heteroaryl; orR 3 and R 3 '' together form a ring structure;R 3 "" is hydrogen, lower alkyl or an aryl; orR 2 and R 3 "" together form a lower alkylene group --(CH 2) n -- wherein n is an integer of 1, 2 or 3; orR 2 and R 3 "" together form a group represented by the formula: --(CH 2) p --Ar-- or --Ar--(CH 2) p --, respectively, wherein p is zero or an integer of 1 or 2, and Ar is an arylene or heteroarylene;C( X) is C( O), C( S), C( NH), C( N-lower alkyl); C NH--OH, or CH 2 ;Y is a direct bond, --NH--, a lower alkyl-N, an oxygen atom, or methylene; orC( X) is CHOH and Y is a direct bond or methylene;R 4 is --(CH 2) s --Ar'' wherein s is zero or an integer of 1, 2 or 3; and Ar'' is an aryl, or a heteroaryl; andR 5 is carboxy, substituted or unsubstituted carboxamide, PO(OH) 2, tetrazole, CH 2 OH, CN, or hydrogen;and salts thereof.
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- Synthesis and &β-adrenoceptor blocking activity of some aryloxy- and benzyloxy-propanolamines
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4-(3-Thienyl)phenoxypropanolamines 9a-n and 4-(3-thienyl)benzyloxypropanolamines 10a-n have been synthesised starting from 3-(p-tolyl)thiophene (1) and 3-(4-methoxyphenyl)thiophene (2).Compound 1 on treatment with N-bromosuccinimide in refluxing CCl4 using dibenzoylperoxide or 2,2'-azobis(2-methylpropionitrile) as a catalyst gives 4-(3-thienyl)benzyl bromide (4) which on refluxing with AcOK/AcOH yields 4-(3-thienyl)benzyl acetate (5).The acetate 5 on hydrolysis furnishes 4-(3-thienyl)benzyl alcohol (6).Further, 3,4-(methoxyphenyl)thiophene (2) on demethylation yields 4-(3-thienyl)phenol (3).The phenol (3) and alcohol 6 on treatment with epichlorohydrin undergo alkylation to give 2,3-epoxy-4-(3-thienyl)phenoxypropane (7) and 2,3-epoxy-4-(3-thienyl)benzyloxypropane (8) respectively which on condensation with various amines in refluxing ethanol furnish 4-(3-thienyl)phenoxypropanolamines (9) and 4-(3-thienyl)benzyloxypropanolamines (10) respectively.Compounds 9 and 10 have been evaluated for their β-adrenergic blocking activity and a few of them shown moderate β-adrenergic blocking activity.
- Marwah, A. K.,Marwah, Padma,Rao, G. Shankar,Trivedi, B. S.,Rao, B. E.,et al.
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p. 197 - 200
(2007/10/02)
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- Benzo-fused lactams promote release of growth hormone
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There are disclosed certain novel compounds identified as benzo-fused lactams STR1 which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.
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