A convenient one-pot preparation and applications of high loading benzhydrylamine solid phase linkers

A rapid and convenient one-pot route to solid supported benzhydrylamine linkers with high chemical loading is described. Such linkers possess differing levels of acid lability, which could be exploited in solid phase synthesis applications. They have also been utilised to prepare novel and potentially useful N-methylated derivatives. We also report an effective on-resin purification strategy for reductive amination, which is facilitated by the varying acid lability of resin-linked secondary amines or tertiary amine by-products.