- Synthesis method of 1-piperidin-4-yl-1,3-dihydro-imidazol[4, 5-b]pyridine-2-one
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The invention discloses a synthesis method of 1-piperidin-4-yl-1,3-dihydro-imidazol[4, 5-b]pyridine-2-one. With 4-piperidone hydrochloride as a start raw material, the synthesis method comprises the following steps: reacting to generate N-t-butyloxycarboryl-4-piperidone and 4-amino-1-t-butyloxycarboryl piperidine; and finally, performing a Curtius rearrangement reaction between 2-(4-amino)piperidyl-3-pyridine carboxylic acid and an azide reagent to obtain a compound 1-piperidin-4-yl-1,3-dihydro-imidazol[4, 5-b]pyridine-2-one of formula V. The synthesis method has the advantages of low cost, easiness in operation, safety, greenness and high yield and can be applied to industrial expanded production.
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- Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: Optimization of the 4-substituted piperidine
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In our continuing effort to identify CGRP receptor antagonists for the acute treatment of migraine, we have undertaken a study to evaluate alternative 4-substituted piperidines to the lead dihydroquinazolinone 1. In this regard, we have identified the piperidinyl-azabenzimidazolone and phenylimidazolinone structures which, when incorporated into the benzodiazepine core, afford potent CGRP receptor antagonists (e.g., 18 and 29). These studies produced a potent analog (18) which overcomes the instability issues associated with the lead structure 1. A general pharmacophore for the 4-substituted piperidine component of these CGRP receptor antagonists is also presented.
- Burgey, Christopher S.,Stump, Craig A.,Nguyen, Diem N.,Deng, James Z.,Quigley, Amy G.,Norton, Beth R.,Bell, Ian M.,Mosser, Scott D.,Salvatore, Christopher A.,Rutledge, Ruth Z.,Kane, Stefanie A.,Koblan, Kenneth S.,Vacca, Joseph P.,Graham, Samuel L.,Williams, Theresa M.
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p. 5052 - 5056
(2007/10/03)
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- Dipeptides which promote release of growth hormone
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Compounds of formula (I) are growth hormone releasing peptide mimetics which are useful for the treatment and prevention of osteoporosis. STR1
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