3-Amino-1H-pyrazolo[4,3-c]pyridin-4(5H)-ones represent a potentially attractive heteroaromatic scaffold for drug-discovery chemistry. In particular, the arrangement of hydrogen bond donor and acceptor groups in the bicyclic core can fulfil the requirements for ATP competitive binding to kinase enzymes. Efficient and regioselective routes from simple starting materials to novel functionalised 3-amino-1H-pyrazolo[4,3-c]pyridin-4(5H)-ones and related 3-amino-2H-pyrazolo[4,3-c]pyridines were explored and adapted for parallel synthesis, resulting in a library of compounds suitable for screening against kinases and other cancer drug targets. Methods for substituent variation at five distinct positions around the bicyclic core were devised to generate sets of compounds containing two- or three-point diversity.

3-氨基-1 H-吡唑并[4,3- c ]吡啶-4（5 H）-ones代表了一种潜在的有吸引力的杂芳骨架，用于药物发现化学。特别地，双环核心中氢键供体和受体基团的排列可以满足ATP竞争性结合激酶的要求。从简单的原料到新型功能化的3-氨基-1 H-吡唑并[4,3- c ]吡啶4-4 （5 H）-ones和相关的3-氨基-2 H-吡唑并[4,3- ]的高效和区域选择性途径C探索了吡啶并使其适于平行合成，从而形成了适合于针对激酶和其他抗癌药物靶标进行筛选的化合物文库。设计了在双环核周围五个不同位置取代基变化的方法，以生成包含两点或三点多样性的化合物。