Loading patent…
AssigneesInstytut Przemyslu Farmaceutycznego, Centrum Baden Molekularnych i Makromolekularnych -PAN, Instytut Immunologii I Terapii Doswiadczalnej Pan
InventorsWojciech J. Stec, Czeslaw Radzikowski, Wieslaw Szelejewski, Ryszard Kinas, Konrad Misiura, Grzegorz Grynkiewicz, Jacek Grodner, Halina Kusnierczyk, Andrzej Kutner, Slawomira Pilichowska
Estimating the term…
Process for production of derivatives of 1,3,2-oxazaphosphorinane of general formula 1, ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen atom or 2-halogenoalkyl group, and R.sub.1 and R.sub.2 are not at the same time hydrogen atoms, and X represents halogen atom is based, according to the invention, on the reduction of the respective 3-halogenoacyl derivatives of 1,3,2-oxazaphosphorinane of general formula 2, ##STR2## wherein the substituents have the above given meaning. The reduction is accomplished with the use of sodium borohydride in the presence of boron trifluoride etherate. Derivatives that are prepared by the procedure described here demonstrate antitumor activity.
A process for the preparation of the derivatives of 1,3,2-oxazaphosphorinane of general formula 1, ##STR5## wherein R.sub.1 and R.sub.2 represent hydrogen atom or 2-halogenoalkyl group and R.sub.1 and R.sub.2 are not at the same time hydrogen atoms, and X represents halogen atom, which comprises reduction of the compound of general formula 2, ##STR6## wherin substituents have the above given meaning, with sodium borohydride, used in a stoichiometric amount in the presence of boron trifluoride etherate in the medium of neutral ether type organic solvent, and isolation and purification of the product by a known method.
Dependencies are inferred from the claim text.