Abstract:
:A novel parallel medicinal chemistry (PMC)-enabled synthesis of 1H-pyrazolo[3,4-d]pyrimidines employing condensation of easily accessible N-pyrazolylamides and nitriles has been developed. The presented studies describe singleton and library enablements that allowed rapid generation of molecular diversity to examine C4 and C6 vectors. This chemistry enabled access to challenging alkyl substituents, expanding the overall chemical space beyond that available via typical C(sp2)-C(sp2) coupling and SNAr transformations. Furthermore, monomer group interconversions allowing the use of larger and more diverse amides and carboxylic acids as precursors to nitriles are discussed.
journal_name
ACS Comb Scijournal_title
ACS combinatorial scienceauthors
Shah AA,Chenard LK,Tucker JW,Helal CJdoi
10.1021/acscombsci.7b00116subject
Has Abstractpub_date
2017-11-13 00:00:00pages
675-680issue
11eissn
2156-8952issn
2156-8944journal_volume
19pub_type
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