- Method for synthesizing ethyl 4-[(2-amino-4-chloro)phenyl]-amino-N-piperidinecarboxylate
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The invention provides a method for synthesizing ethyl 4-[(2-amino-4-chloro)phenyl]-amino-N-piperidinecarboxylate. A reaction route of the method is as described in the specification. The invention has the following beneficial effects: 1, the novel synthetic method is designed in the invention for preparation of a domperidone intermediate with a structure as shown in a formula (DP-2) and is implemented, and the method uses easily available raw materials and is high in safety coefficient, simple in reaction and beneficial for realizing of large-scale industrial production; and 2, no special production equipment is need in the method, industrial scale-up production can be easily carried out, and production cost for the domperidone intermediate is greatly lowered, so production cost for domperidone is substantially reduced.
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Paragraph 0007; 0020-0022; 0026-0028; 0030-0032; 0034-0036
(2018/09/08)
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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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- Neuroleptic n-oxacyclyl-alkylpiperidine derivatives
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Neuroleptically active compounds of the formula STR1 wherein R6 and R10 are --H or CH3 ; R7 and R8 are independently --H, --F, --Cl, or --CH3 ; and R9 is --F, --Cl, --CH3, or --OCH3.
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