79098-75-2Relevant articles and documents
An efficient synthesis of the piperidinyl dihydroquinazolinone (PDQ) fragment of olcegepant
Habay, Stephen A.,Miller, Julia M.,Bowler, Matthew M.,Manchak, Randi,Thomas, John Z.
, p. 3389 - 3391 (2018)
Olcegepant is one of the most potent and selective small molecule CGRP antagonists for the treatment of migraine headaches. Herein, we describe a new and efficient synthesis of the key piperidinyl dihydroquinazolinone (PDQ) fragment of olcegepant. PDQ plays a key role in the activity of CGRP antagonists. Primary improvements over existing methods include a high-yielding reductive amination step, greater overall yield, and operational simplicity. Coupling of PDQ to a D-tyrosine derivative effectively produced over one half of the total molecular structure of olcegepant. A unique tandem deprotection-nucleophilic addition sequence was also applied to the coupling of Fmoc-PDQ with phenyl isocyanate.
DIPHENYLBUTYPIPERIDINE AUTOPHAGY INDUCERS
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, (2011/12/02)
Autophagy inducing compounds, methods of their preparation and use, and kits containg said compounds are disclosed herein.
Process for preparing 1- [N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine
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Page/Page column 5, (2010/02/13)
The present application relates to a process for preparing the CGRP-antagonist 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine of formula by means of which this compound can be prepared in large amounts, in high yields and with high purity.