6943-97-1Relevant academic research and scientific papers
AMINE COMPOUND AND PHARMACEUTICAL USE THEREOF
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Page/Page column 56, (2010/04/25)
Provided is a novel amine compound represented by the following formula (I) having a superior peripheral blood lymphocyte decreasing action and superior in the immunosuppressive action, rejection suppressive action and the like, which shows decreased side effects of, for example, bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof. wherein each symbol is as defined in the specification.
Inhibitors of prenyl-protein transferase
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, (2008/06/13)
The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
SUBSTITUTED 1H-IMIDAZOLES
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, (2008/06/13)
Substituted 4-(1,2,3,4-tetrahydro-1-naphthalenyl)-1H-imidazoles and 4-(2,3-dihydro-1H-inden-1-yl)-1H-imidazoles, their optical isomers and their racemic mixtures, their salts, methods for preparing them and therapeutic compositions containing them. These compounds have the general formula STR1 wherein n=1 or 2,R 1, R. sub.2, R 3 and R 4 =hydrogen, halogen, hydroxyl C 1-C 4 alkyl or C 1-C 4 alkoxy,R 5 = hydrogen of C 1-C 4 alkyl with the proviso that R 1, R. sub.2, R 3, R. sub.4 and R 5, cannot simultaneously be hydrogen when n is equal to 2. These new compounds exhibit anti-ischemic and anti-hypertensive activities.
Syntheses of Tetrahydronaphthalenes. Part II
Parlow, John J.
, p. 3297 - 3314 (2007/10/02)
Syntheses utilizing the cyclodehydration method to prepare novel tetrahydronaphthalenes substituted with functional groups at each position of the aromatic ring and various alkyl groups at the 1-position of the non-aromatic ring are described.
Furan Derivatives. Part 10. Synthesis of Cycloheptabenzofuran
Horaguchi, Takaaki,Hasegawa, Eietsu,Shimizu, Takahachi,Tanemura, Kiyoshi,Suzuki, Tsuneo
, p. 365 - 369 (2007/10/02)
Cycloheptabenzofuran 2 was synthesized by heating (5-oxo-5H-benzocyclohepten-4-yloxy)acetic acid 16 with sodium acetate in acetic anhydride or by photocyclization of 16 in acetonitrile.Several reactions of cycloheptabenzofuran 2 were examined.Protonation of 2 with trifluoroacetic acid occurred at the 2-position to give a tropylium ion 17.Catalytic hydrogenation of 2 with palladium on charcoal proceeded smoothly to give tetrahydrocycloheptabenzofuran 18.The Diels-Alder reaction of 2 with tetracyanoethylene produced an adduct 19.Formylation of 2 with phosphorus oxychloride and dimethylformamide occurred easily at the 2-position to afford compound 20.Cycloheptabenzofuran 2 has both properties of heptafulvene and benzofuran.
The Preparation of 2,3,3a,4,5,6-Hexahydro-8-methoxy-1H-phenalene
Maskill, H.
, p. 1739 - 1742 (2007/10/02)
The previously unknown methoxy substituted benzene derivative 2,3,3a,4,5,6-hexahydro-8-methoxy-1H-phenalene (3a) has been prepared by two routes.One starts from 6-methoxy-α-tetralone (4a) and involves a single 3-carbon extension and cycization of the alcohol (7b); the other starts from 3-(3-methoxyphenyl)propanoic acid (5a) and proceeds via a 4-carbon extension and a double cyclization of the diol (10).
Antifertility Agents: Part XLVI - Synthesis and Activity of 1,2-trans-1--2-phenyl-7-methoxybenzosuberan
Sangwan, Naresh K.,Prasad, Mohan,Rastogi, Shri Nivas,Jehan, Qaiser,Setty, B. S.
, p. 832 - 837 (2007/10/02)
Treatment of 1-bromo-3-(m-methoxyphenyl)propane (2) with p-methoxydesoxybenzoin and benzyl cyanide yields 1,5-diaryl-2-phenylpentanone (5) and 2,5-diarylpentanenitrile (6) respectively.Demethylation of 5 gives 1-(p-hydroxyphenyl)-3-(m-methoxyphenyl) (7) and 1-(p-hydroxyphenyl)-3-(m-hydroxyphenyl)-(8)-2-phenylpentanones which on acetylation afford mono- and di-acetates 9 and 10 respectively.Attempted cyclisation of 7 and 9 with p-TsOH fails to give the desired 1,2-diarylbenzosuber-1-ene (11).In another approach, 6 is hydrolysed to yield the acid 12 which on treatment with PPA gives 2-phenylbenzosuber-1-one (13) while with PCl5-SnCl4 it gives a mixture of 13 and 1-chloro-2-phenylbenzosuber-1-ene (14).Reaction of 13 and p-(trimethylsilyloxy)phenylmagnesium bromide gives 11 in a low yield.Alternatively, 13 is reduced with NaBH4 to give a cis-/trans-mixture of suberols 15a,b which on treatment with PhOH-AlCl3 yield mainly 1,2-trans-1-(p-hydroxyphenyl)-2-phenyl-7-methoxybenzosuberan (18) along with 2-phenylbenzosuber-1-ene (16) and traces of 1-(o-hydroxyphenyl)-2-phenylbenzosuberan (18a).Acetylation of 18 gives the acetate 19 and alkylation of 18 furnishes the desired compound, 1,2-trans-1--2-phenyl-7-methoxybenzosuberan (III, 20).The compound 20 prevents pregnancy in rats at 0.2 mg/kg daily oral dose on days 1-5 post-coitum or at a single oral dose of 1.5 mg/kg on day 1 post-coitum.At 0.2 mg/kg dose, it is 1000 times less estrogenic than ethinylestradiol and is antiestrogenic at single day contraceptive dose.
Intramolecular Alkylation of Phenols. Part 5. A Regiospecific Anionic Ring Closure of Phenols via Quinone Methides
Murphy, William S.,Wattanasin, Sompong
, p. 1567 - 1577 (2007/10/02)
The bis-magnesium salts of the triols (6a) and (6h) cyclise when heated in benzene with high ortho-regiospecificity to the corresponding bis-phenols (7) and (8).The triols (6k) and (6o) under the same conditions cyclise with high para-regiospecificity to the corresponding bis-phenols (7) and (8).Both (6a) and (6h) cyclise via o-quinone methides, and (6k) and (6o) via p-quinone methides.Results from the use of, inter alia, 18-crown-6, indicate that the high ortho-regiospecificity of the cyclisation of (6a) and (6h) is due to intramolecular Mg(II) bridging of the intermediate o-quinone methides.The high para-regiospecificity of cyclisation of (6k) and (6o) is due to steric hindrance towards o-cyclisation of the intermediate p-quinone methides presented by the Mg(II) cation.The unexpected facility with which (6a) and (6k) undergo ring closure is discussed.
Production of unsaturated carbocyclic ketones
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, (2008/06/13)
Preparation of α,β-unsaturated carbocyclic ketones by reacting an enol lactone with a carbanion generated by treatment of a methylphosphonate or a mono-substituted methylphosphonate with base.
