Erno Mohacsi

A Convenient Preparation of Methyl Esters from Carboxylic Acids

Abstract A facile procedure for the preparation of methyl esters from carboxylic acids under neutral conditions is described.

A New Synthetic Method for the Preparation of Tert-Butyl Aryl Ethers

Abstract A facile synthesis for the preparation of tert-butyl aryl ethers from phenols under basic conditions is described.

A Convenient Method for the Synthesis of Cyclic Imino Ethers

Abstract A facile procedure for the preparation of cyclic imino ethers from thiocaprolactam and chloroformates is described.

Studies on the Metabolism of 3-O-tert.-Butylmorphine, a New Morphine Derivative, by the Rat

1. The O-dealkylation of 3-O-tert.-butylmorphine, a new derivative of morphine, has been compared to the O-dealkylation of codeine by the rat. Rats were given either 3-O-tert.-butylmorphine or codeine intraperitoneally and 24 h urine samples were collected and analysed for morphine by a quantitative gas chromatographic procedure. With codeine, about 7% of the dose was excreted as morphine. In contrast, about 0.3% of a dose of 3-O-tert.-butylmorphine was recovered from urine as morphine. These results indicate that, unlike codeine, 3-O-tert.-butylmorphine is not O-dealkylated to any appreciable extent by the rat.2. Three metabolites of 3-O-tert.-butylmorphine have been recovered from rat urine, resolved by gas chromatography and identified by mass spectroscopy as 3-O-tert.-butylnormorphine, 3-O-(2-hydroxymethyl-2-propyl)morphine and 3-O-(2-hydroxymethyl-2-propyl)normorphine. The identities of the last two metabolites were confirmed by comparison of their mass spectra with the mass spectra of synthetic refe...

A New Synthetic Method for the Preparation of N,N-Dimethylformamide DI-Tert-Butyl Acetal

Abstract A new synthetic method for the preparation of N,N-dimethylformamide di-tert-butyl acetal by acid catalyzed transacetalization of readily available N,N-dimethylformamide dimethyl acetal is described.

(−)‐2‐Hydroxy‐N‐cyclopropylmethylmorphinan: Radioimmunoassay and pharmacokinetic profile

The pharmacokinetic profile of (−)‐2‐hydroxy‐N‐cyclopropylmethylmorphinan (HCMM), a narcotic antagonist and analgesic, has been evaulated in man following administration of 25 to 50 mg of the drug orally and 10 to 15 mg intramuscularly. A specific radioimmunoassay procedure was developed for the determination of HCMM in plasma and urine. The drug had a mean “apparent” elimination half‐life in plasma of about 11 hr following both routes of administration. A mean of 47% of the oral dose was excreted in the urine as unconjugated and conjugated HCMM and only 5% of the dose was excreted as intact HCMM. In one subject studied, the plasma levels of conjugated HCMM were as much as 5‐fold higher than the levels of un conjugated drug. Although there was considerable intersubject variability following both routes of administration, the overall pharmacokinetic parameters suggest that oral and intramuscular doses are bioequivalent.