Merck Patent Gesellschaft MIT Beschrankter Haftung

Merck Patent Gesellschaft MIT Beschraenkter Haftung

Michael Casutt

Eike Poetsch

Michael Schwarz

Ulrich Heywang

Ingeborg Stein

Roland Martin

Jurgen Eckstein

Henning Bottcher

Hartmut Hartner

Richard Kirchlechner

Harry Schwartz

Arno Basedow

Ulrich Fechtel

Thomas Koppe

Willem N Speckamp

Gerald Faller

Gunther Holzemann

Preparation of a D-(+)-biotin intermediate

Triazine derivatives with UV filter properties

Process for preparing 2-arylbenzimidazole-5-sulfonic acids

The invention relates to benzylidene-quinuclidinone derivatives of the formula I ##STR1## in which R.sup.1 is A;

Benzylidenequinuclidinones

Process for the preparation of N-protected dialkyl

2-oxo-5-mercaptomethylimidazolidine-4-ols

The present invention relates to a process for the preparation of heterocyclic compounds which are suitable as intermediates for the preparation of D-(+)-biotin, and to a process for the preparation of D-(+)-biotin itself. The invention further relates to intermediates in this process.

Process for the preparation of a D-(+)-biotin intermediate

The invention relates to a novel process for the preparation of imidazothiazolone derivatives of formula I, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined in the claims, which are suitable for the preparation of D-(+)-biotin.

Process for the preparation of imidazothiazolone derivatives

The invention relates to a process for the preparation of racemic pilosinine derivatives as precursor for the alkaloid pilocarpine of pharmacological importance from a 5-formyl-1-alkylimidazole of the formula I ##STR1## in which R.sup.1 is a straight-chain or branched alkyl chain with 1-6 C atoms which, via the stage of the thioacetal, is added onto .gamma.-crotonolactone.

Pilosinine derivatives

D-(+)-biotin can be prepared from optically active hydantoins of the formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given in Patent claim 1, in a simple, stereospecific manner. Furthermore bicyclic nitriles of the formula XI ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given represent precious intermediate products and educts of a multitude of possibilities to synthesize optically active D-(+)-biotin.

Process for the preparation of D-(+)-biotin

Process for the preparation of 5-membered nitrogen containing

Optically active hydantoins of the formula I ##STR1## wherein X, Y, R.sup.1, R.sup.2 and R.sup.3 have the meaning given in Patent claim 1, are useful intermediate products for the preparation of D-(+)-biotin.

Optically active hydantoins

D-(+)-biotin can be prepared from optically active hydantoins of the formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given in Patent Claim 1, in a simple, sterospecific manner. Furthermore bicyclic nitriles of the formula XI ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given represent precious intermediate products and educts of a multitude of possibilities to synthesize optically active D-(+)-biotin.

D-(+)-Biotin can be prepared from optically active hydantoins of the formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given in patent claim 1, in a simple, stereospecific manner. Furthermore bicyclic nitriles of the formula XI ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given represent precious intermediate products and educts of a multitude of possibilities to synthesize optically active D-(+)-biotin.

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Heppenheim, Germany

Michael Casutt