75693-20-8Relevant academic research and scientific papers
Piperazine compounds
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Page/Page column 14, (2008/06/13)
A compound selected from those of formula (I): wherein: R1, R2, R3 and R4, which may be the same or different, each represent an atom or group selected from hydrogen, halogen, alkyl, alkoxy, phenyl and cyano, X represents a bond, an oxygen atom or a group selected from —(CH2)m—, —OCH2— and —NR5—, wherein m represents 1 or 2, and R5 is as defined in the description, Y represents an oxygen atom or a group selected from NR7 and CHR8, wherein R7 and R8 are as defined in the description, Z represents a nitrogen atom or a CH group, n represents 1 or 2, Ak represents an alkylene chain, Ar represents an aryl or heteroaryl group, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid. Medical products containing the same which are useful in the treatment of conditions requiring a serotonin reuptake inhibitor and/or NK1 antagonist.
AROMATIC SUBSTITUENT EFFECT ON THE STEREOSELECTIVITY OF THE ACID-INDUCED RING OPENING OF 1,2-EPOXIDES DERIVED FROM 3,4-DIHYDRONAPHTHALENE. IMPORTANCE OF THE REACTIVE CONFORMATIONS FOR THE STEREOSELECTIVITY.
Chini, Marco,Crotti, Paolo,Minutolo, Filippo,Martinelli, Adriano,Micali, Eugenio
, p. 27 - 34 (2007/10/02)
The stereochemistry of the acid-induced ring opening reactions (hydrolysis, methanolysis and trichloroacetolysis) of 1,2-epoxides derived from ring substituted 3,4-dihydronaphthalene has been examined.In every case, a satisfactory Hammett-type linear correlation was found between the diastereoselectivity of the reaction and the ?+ constant of the aromatic substituent.The stereoselectivity of the opening reaction turned out to be largely driven by the reactive conformation of the epoxide and/or of the opening process intermediates.
Synthesis and Immunological Activity of 5,6,6a,8,9,11a-Hexahydronaphthimidazothiazoles and 5,6,6a,9,10,11a-Hexahydronaphthimidazothiazoles
Saito, Masahiko,Kayama, Yasutaka,Watanabe, Tamaki,Fukushima, Hisashi,Hara, Takeshi,et al.
, p. 1364 - 1372 (2007/10/02)
A series of 5,6,6a,8,9,11a-hexahydronaphthimidazothiazoles (17 and 20) and 5,6,6a,9,10,11a-hexahydronaphthimidazothiazoles (18) has been synthesized with cis- and/or trans-1,2-diamino-1,2,3,4-tetrahydronaphthalenes (12) as the key intermediates and subsequently evaluated for immunological activity (effects on antibody formation and delayed-type hypersensitivity reaction).Among the compounds tested, trans-5,6,6a,8,9,11a-hexahydronaphthimidazo(2,1-b>thiazole (trans-17a) and (+/-)-5,6,6aβ-8,9,11aα-hexahydro-8β-hydroxy-9β-methyl-8α-phenylnaphthimidazothiazole (20a) showed the largest immunological activity in mice with a magnitude comparable to that of levamisole and were found to be considerably less toxic than levamisole in an acute toxicological study.The structures of 18a and 20a were determined by X-ray crystallography.
