| 摘要 |
<p>A disclosed process for the preparation of N-(n- -alkanesulphonyl)-O-[4-(4-piperidinyl)alkyl]-(L)-tyrosine and the derivatives thereof is characterised in that 4-picoline reacts with butyllithium and brominated tetrahydropyan thus forming a compound of formula (a); said compound (a) reacts with hydrochlorid gas in ethanol and is subsequently neutralised in a mixture of triethylamine and tetrahydrofuran to form a compound of formula (b), whilst the compound of formula (b) reacts with N-(n-alkanesulphonyl)-(L)-tyrosine methylester in the presence of triphenylphosphine, tetrahydrofuran and diisopropyl azodicarboxylate and then it reacts with lithium hydroxide in tetrahydrofuran, with methanol and water to form a compound of formula (c) which is further subjected to a selective hydrogenation in the presence of a palladium catalyst in acetic acid to form N-(n-alkanesulphonyl)-O-[4-(4-piperidinyl)-alkyl]- -(L)-tyrosine, or the product is converted to its additional salt with an acid.</p> |
