| 摘要 |
In the present invention, there are disclosed lipophilic analogs of protected amino acids of the general formula I, in which Ri1 a Ri2 represent independently on each other groups such as H, alkyl containing 3 to 40 carbon atoms, and PG represents Fmoc, Boc or Cbz protecting group. The lipophilic analogs can be prepared by two-stage synthesis resulting from a protected N,O-ditrimethyl silyl derivative II and a corresponding fatty acylation agent III, wherein LG denotes a halogen or another activating group (reaction 1). The product of this reaction is an intermediate IV, which can be transferred by an easy hydrolysis and in dependence on reaction conditions to the substance I (reaction 2). Thus, the product I is obtained in a high yield and purity without occurrence of oligomeric and degradation side products. The preparation process of the present invention can be used for the synthesis of substances in multi-kg amounts for pharmaceutical production. |
