Metabolism of the local anaesthetic fomocaine by rat liver mitochondria
Fomocaine (Erbocain) is metabolized by different routes in rat and beagle. By highly purified rat liver mitochondria it was metabolized to its N-oxide only. The N-oxide was reduced to fomocaine by a reductase localised in the matrix or in the inner membrane of the mitochondria. C-Hydroxylation with subsequent conjugation reactions as well as oxidative N- or O-dealkylation found in intact animals were not observed in mitochondria.
Blume,Oelschlaeger
p. 1731 - 1735
(2007/10/02)
On a novel fomocaine synthesis: 10th communication: on synthesis of new compounds with local anaesthetic activity
4 [3 (4 Phenoxymethyl phenyl) propyl] morphine (fomocaine, Erbocain) is a very active topical local anesthetic with low toxicity. A new synthesis starting from 4-phenoxy-methyl-benzonitrile, via a modified Willgerodt-Kindler reaction, is reported. The yield is of the same order as with the known technical process starting from 3-phenylpropanol. The distinct advantage of the new procedure is the avoidance of the C-chloromethylation of 3-phenylpropylchloride during which process the o-chloromethyl derivative is also formed, and this cannot be separated by fractional distillation.
Oelschlaeger,Iglesias-Meier,Goetze,Schatton
p. 1625 - 1628
(2007/10/05)
Synthesis of new compounds with local anesthetic action. 3. Preparation of the local anesthestic aminoether N-[3-(4-phenoxymethylphenyl)-propyl] morpholine & the relation between toxicity & the basic components of N-[3-(4-phenoxymethylphenyl)-propyl]-amines].
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OELSCHLAGER
p. 313 - 321
(2007/10/04)
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