Microwave-assisted, solid-phise synthesis of a chiral 1,2,3,4-tetrahydroquinoline library

作者：Lesma Giordano; Danieli Bruno; Lodroni Francesco; Passarella Daniele; Sacchetti Alessandro; Silvani Alessandra^*

来源：Combinatorial Chemistry & High Throughput Screening, 2006, 9(9): 691-701.

DOI：10.2174/138620706778700134

• combinatorial chemistry
• solid phase synthesis
• microwave
• tetrahydroisoquinoline

The synergy of a solution-phase preparation of scaffolds with a solid-phase combinatorial synthesis let to develop an efficient route to a small library of chiral, highly functionalized tetrahydroisoquinolines. Both loading on the Merrifield resin and the key acid-catalyzed Pictet-Spengler condensation were efficiently promoted by microwave irradiation. The library was designed such that up to five points of diversity would be potentially introduced, making the strategy in principle suitable for generation of a large number of compounds.

• 出版日期2006-11