L‐Cα‐t‐Butylglycine (Bug), its amide, methyl ester, and Nα‐t‐butoxycarbonyl derivative were prepared by an asymmetric synthesis, and the Hansch side‐chain hydrophobic (lipophilicity) parameter determined. A new enkephalin analogue, H · Tyr‐D‐Ala‐Gly‐Phe‐Bug · NH2 was synthesized which is pharmacologically active in two in vitro assays and strongly resistant against a number of enzymes in vitro.
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Fauchère et al. (1980) studied this question.
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