참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Acetone | HCID 180 | — |
| 반응물 | Diethyl Ether | HCID 3283 | — |
| 반응물 | N-Methyl-D-glucamine | HCID 8567 | — |
| 반응물 | Amphotericin B | HCID 5280965 | — |
| 용매 | Dimethyl Sulfoxide | HCID 679 | — |
| 생성물 | Amphoglucamine | HCID 6449900 | 137% |
반응 단계
19.7 g of amphotericin B with a specific biological activity of 750 mcg/mg (ED/mg) and 14.7 g of meglumine with the content of 1-deoxy-1-(methylamino)-glucitol of at least 99% are dissolved in 100 ml of dimethylsulphoxide at a temperature within the range of from 50° to 60° C and stirred for 10 minutes. The resulting solution is added with a 7-fold volume of a mixture of acetone with diethyl ether (in a volumetric ratio of 1:1). The precipitate is filtered off, washed with the same mixture of acetone with diethyl ether, and dried at 20° C under a residual pressure of 100 mm Hg to give 32.7 g of amphoglucamine with a specific biological activity of 440 mcg/mg (ED/mg) which corresponds to the yield of 96% of amphoglucamine based on the activity of the starting amphotericin B.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US04007166 |
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| 출처 데이터셋 | uspto-grants-1977_02 |
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| ORD ID | ord-d412bd9616854897b1590d92f597f00c |
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| 출처 메모 | uspto-grants-1977_02 |
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