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KMID : 1059519990430030294
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Journal of the Korean Chemical Society
1999 Volume.43 No. 3 p.294 ~ p.301
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Studies on the Synthesis of Geminal Bisphosphono Amine Derivatives Using Pentacovalent Oxaphospholenes
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Lee Mi-Young
Jung Kang-Yeoun
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Abstract
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Geminal bisphosphonates have been well known to be effective inhibitors of various calciumrelated disorders such as Paget's disease, hypercalcemia of malignancy, and osteoporosis. To synthesize bisphosphonates, we have used the pentacovalent oxaphospholene prepared from methyl vinyl ketone and triethyl-phosphite. Υ-Ketobisphosphonates are obtained by bromination, applied Westheimer reaction, and hydrolysis of synthesized oxaphospholene. This compound was converted to the N-alkylated Υ-aminobisphosphonates by the reductive amination. Conversion of the resulting secondary amine to the tertiary one, followed by introduction of the second alkyl group on the nitrogen, was led to the synthesis of new N,N'-dialkylated Υ-aminobisphosphonates.
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