53786-45-1Relevant academic research and scientific papers
Method for synthesizing ethyl 4-[(2-amino-4-chloro)phenyl]-amino-N-piperidinecarboxylate
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Paragraph 0007; 0020; 0023; 0029; 0033; 0037, (2018/09/08)
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.
Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: Optimization of the 4-substituted piperidine
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.
, p. 5052 - 5056 (2007/10/03)
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.
Neuroleptic n-oxacyclyl-alkylpiperidine derivatives
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, (2008/06/13)
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.
