21413-70-7Relevant academic research and scientific papers
Chemo- and stereoselective synthesis of benzocycloheptene and 1-benzoxepin derivatives as α-sympathomimetic and anorexigenic agents
Tandon, Vishnu K.,Singh, Kunwar A.,Awasthi, Anoop K.,Khanna,Lal, Bansi,Anand, Nitya
, p. 2867 - 2870 (2004)
The synthesis and pharmacological evaluation of cis- and trans-6-amino-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ols 4a-c and 5a-c and cis- and trans-4-amino-2,3,4,5-tetrahydro-1-benzoxepin-5-ols 4d-f and 5d-f were carried out. Chemo- and stereoselective synthesis of 5a-f was achieved by reduction of corresponding α-amino ketones 3a-f with LiAl(t-BuO) 3H. cis-4-Amino-2,3,4,5-tetrahydro-1-benzoxepin-5-ol 4d and trans-4-amino-2,3,4,5-tetrahydro-1-benzoxepin-5-ol 5d exhibited marked anorexigenic activity in mice at a dose of LD50 800 and 500mg/kg and ED50 75 and 55mg/kg, respectively, while the analog cis-2,3-dihydroxy-6-amino-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol 8 showed typical α-sympathomimetic activity.
Benzocycloalkane derivatives and production thereof
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, (2008/06/13)
Benzocycloalkane derivative of the formula wherein R is a hydrogen atom or a hydrocarbon residue, which may optionally have one or more substituents, Ar is an aromatic group, X is an oxygen or sulfur atom, l is 0 or 1, m is 3 to 6 and n is 0 to 2, wherein the ring A and the group Ar each may optionally have one or more substituents, with the proviso that compounds are excluded, wherein Ar is whereby Rxand Ryare independently selected from alkyl or alkoxy of from one to seven carbon atoms, or its pharmaceutically acceptable salt, which is useful as inhibitors for acyl-CoA : cholesterolacyltransferase.
