Organic compounds -- part of the class 532-570 series – Organic compounds – Phosphorus esters
Patent
1988-06-09
1990-03-13
Sutto, Anton H.
Organic compounds -- part of the class 532-570 series
Organic compounds
Phosphorus esters
C07F 924
Patent
active
049084640
ABSTRACT:
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.
REFERENCES:
K. Pankiewicz et al.; Synthesis and Absolute Configuration Assignment of Enantiomeric Forms of Ifosphamide, Sulfosphamide, and Trofosphamide; Dec. 19, 1979, of Journal of the American Chemical Society/101:26; pp. 7712-7718.
Wagner et al., "Synthetic Organic Chemistry", (1953), p. 660.
Grodner Jacek
Grynkiewicz Grzegorz
Kinas Ryszard
Kusnierczyk Halina
Kutner Andrzej
Centrum Baden Molekularnych i Makromolekularnych -PAN
Instytut Immunologii i Terapii Doswiadczalnej -PAN
Instytut Przemyslu Farmaceutycznego
Sutto Anton H.
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