Amersham International Plc

Instytut Immunologii I Terapii Doswiadczalnej Pan

Instytut Przemyslu Farmaceutycznego

Centrum Baden Molekularnych I Makromolekularnych -pan

Konrad Misiura

Michael John Gait

Andrzej Kutner

Wieslaw Szelejewski

Wojciech J Stec

Grzegorz Grynkiewicz

Czeslaw Radzikowski

Jacek Grodner

Halina Kusnierczyk

Slawomira Pilichowska

Ryszard Kinas

Phosphoramidite derivatives of formula (V), ##STR1## wherein X is biotin and Y is a protecting group. There may be a linker arm, of variable length, between X and the rest of the molecule. Examples of the protecting group Y include 4,4'-dimethoxytrityl, trifluoroacetyl and fluorenylmethoxycarbonyl (Fmoc). The phosphoramidite derivatives are useful in single or multiple labelling of synthetic oligonucleotides. Process for the preparation of these phosphoramidite derivatives are also disclosed.

Phosphoramidite derivatives, their preparation and the use thereof in

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.

Process for the production of 1,3,2-oxazaphosphorinanes

Growing community of inventors

Lodz, Poland

Konrad Misiura