Preparation of pyrimido[4,5-d]azepine derivatives as 5-HT2C agonists. Andrews, M., D., Blagg, J., Brennan, P., E., Fish, P., V., Roberts, L., R., Storer, R., I., & Whitlock, G., A. 2008.
abstract   bibtex   
The title compds. I [R1 = H, alkyl, fluoroalkyl, cycloalkyl, etc.; R2 = (CH2)pPh, CHR6Ph, NR7R8, etc.; R31, R32, R33, R34 = H, alkyl, fluoroalkyl; R6 = alkyl, fluoroalkyl, OH or F; R7 = alkyl, fluoroalkyl, cycloalkyl or fluorocycloalkyl; R8 = alkyl, fluoroalkyl, cycloalkyl, cycloalkylmethyl or fluorocycloalkyl; or NR7R8 = 4-6 membered heterocyclyl optionally comprising 1 further heteroatom selected from O and S (said ring being optionally fused to a Ph ring); p = 1-2; R100 = H or NH prodrug moiety] which act as 5-HT2C agonists, were prepd. E.g., a multi-step synthesis of II, starting from 1-tert-Bu 4-Et 5-oxoazepane-1,4-dicarboxylate and 2-phenylacetamidine, was given. II showed Ki of 72.0 nM when tested for 5-HT2C agonistic activity. Pharmaceutical compn. comprising the compd. I is disclosed. [on SciFinder(R)]
@misc{
 title = {Preparation of pyrimido[4,5-d]azepine derivatives as 5-HT2C agonists},
 type = {misc},
 year = {2008},
 identifiers = {[object Object]},
 keywords = {pyrimidoazepine prepn serotonin 5HT2C receptor ago},
 pages = {180pp.},
 issue = {Copyright (C) 2012 American Chemical Society (ACS). All Rights Reserved.},
 publisher = {Pfizer Limited, UK .},
 revision = {WO 2008117169 A1},
 id = {88574e90-5df6-3709-ba49-990536f85b45},
 created = {2015-10-01T17:18:19.000Z},
 file_attached = {false},
 profile_id = {64f7fb50-d000-335d-a02d-06c5f340a97a},
 last_modified = {2018-09-03T10:20:45.913Z},
 read = {false},
 starred = {false},
 authored = {true},
 confirmed = {true},
 hidden = {false},
 citation_key = {Andrews2008},
 source_type = {Patent},
 notes = {CAPLUS AN 2008:1185770(Patent)},
 private_publication = {false},
 abstract = {The title compds. I [R1 = H, alkyl, fluoroalkyl, cycloalkyl, etc.; R2 = (CH2)pPh, CHR6Ph, NR7R8, etc.; R31, R32, R33, R34 = H, alkyl, fluoroalkyl; R6 = alkyl, fluoroalkyl, OH or F; R7 = alkyl, fluoroalkyl, cycloalkyl or fluorocycloalkyl; R8 = alkyl, fluoroalkyl, cycloalkyl, cycloalkylmethyl or fluorocycloalkyl; or NR7R8 = 4-6 membered heterocyclyl optionally comprising 1 further heteroatom selected from O and S (said ring being optionally fused to a Ph ring); p = 1-2; R100 = H or NH prodrug moiety] which act as 5-HT2C agonists, were prepd. E.g., a multi-step synthesis of II, starting from 1-tert-Bu 4-Et 5-oxoazepane-1,4-dicarboxylate and 2-phenylacetamidine, was given. II showed Ki of 72.0 nM when tested for 5-HT2C agonistic activity. Pharmaceutical compn. comprising the compd. I is disclosed. [on SciFinder(R)]},
 bibtype = {misc},
 author = {Andrews, Mark David and Blagg, Julian and Brennan, Paul Edward and Fish, Paul Vincent and Roberts, Lee Richard and Storer, Robert Ian and Whitlock, Gavin Alistair}
}

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