- A new simple route to N-substituted 2-aminoethylphosphonic acids
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2-Aminoethylphosphonic acid (AEPA) and its N-substituted compounds were prepared by one step reaction using 2-chloroethylphosphonic acid with ammonia and amines (H2NMe, HNMeMe, HNEtEt, H2NPr-n, H2NCH2ph,H2NCH2CH2NH2 and H2N(C=NH)NH2 in a dilute alkaline solution below 20 °C with simple work- up and easy purification. The reaction was accelerated by catalytic amount of potassium iodide. The yield for the reaction products were 35.6 to 48.6% for the KI absence and 78.2 to 88.0% for the KI presence.
- Fu, Xiangkai,Gong, Chengbin,Ma, Xuebing,Wen, Shuying
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- Tanshinone IIA phosphoric acid derivative and synthesis and use thereof as medicine
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The invention discloses a tanshinone IIA phosphoric acid derivative and synthesis and use thereof as a medicine for treatment. In particular, the present invention provides a novel derivative shown as a general formula (I) and a pharmaceutically acceptable salt thereof or a pharmaceutical composition containing the novel derivative shown as the general formula (I), and a method for preparing the novel derivative shown as the general formula (I). The invention also discloses use of the novel derivative, the pharmaceutically acceptable salt thereof or the pharmaceutical composition containing the novel derivative in preparation of medicines for treatment of coronary heart disease, angina, myocardial infarction, viral myocarditis, arrhythmia, cerebrovascular disease, hepatitis, pulmonary heart disease, bronchial asthma, cancer, kidney disease, eye disease, thromboangiitis obliterans, hypertension, fractures, burns, surgical operations or behcet ' s syndrome. On the basis of ensurance of the activity of tanshinone IIA, the novel derivative, the water solubility of the pharmaceutically acceptable salt thereof or the pharmaceutical composition containing the novel derivative can be improved. Compared with tanshinone IIA sodium sulfonate, the stability is improved, and because the acidity of the pharmaceutically acceptable salt thereof or the pharmaceutical composition containing the novel derivative is reduced obviously, injection stimulation can be avoided. All substituents of the general formula (I) are as defined in the specification.
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Paragraph 0067; 0068; 0069; 0070
(2017/04/03)
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- N-alkyl-N-(Aminophenylsulfonyl)-aminoalkylphosphonic acids and salts
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This invention relates to novel N-alkyl-N-(amino-phenylsulfonyl)-aminoalkylphosphonic acids and to processes for their preparation. These compounds are useful as intermediates, especially for the manufacture of dyes containing phosphonic acid groups in th
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- N-alkyl-N-(aminophenylsulfonyl)-aminoalkylphosphonic acids
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This invention relates to novel N-alkyl-N-(amino-phenylsulfonyl)-aminoalkylphosphonic acids and to processes for their preparation. These compounds are useful as intermediates, especially for the manufacture of dyes containing phosphonic acid groups in th
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- SYNTHESES OF D-ERYTHRO-1-DEOXYDIHYDROCERAMIDE-1-SULFONIC ACID AND PHOSPHONOSPHINGOGLYCOLIPID FOUND IN MARINE ORGANISM VIA A COMMON PRECURSOR
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D-Erythro-1-deoxydihydroceramide-1-sulfonic acid, isolated from alkali-stable hydrogenated lipids in a non-photosynthetic marine diatom, Nitzschia alba, and (2S,3R)-N-palmitoyl-1-O--β-D-galactopyranosyl>-D-sphingosine, found in marine snail Turbo cornutus were synthesized via a common precursor (10) starting from galactose.
- Ohashi, Kinji,Kosai, Shunji,Arizuka, Mitsuo,Watanabe, Takashi,Yamagiwa, Yoshiro,et al.
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p. 2557 - 2570
(2007/10/02)
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- AMINATION REDUCTRICE D'ALDEHYDES PHOSPHONIQUES. Un Reexamen
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The reactivity of diethyl-2-oxo ethyl- and 3-oxo propylphosphonates with ammonia, methyl and dimethylamine at pH 7 in the presence of sodium cyanohydridoborate via reductive amination of the carbonyl group has been reexamined.Reactions of diethyl-2-oxoethyl- and 3-oxopropylphosphonates with ammonia give imino-bis-(alkylphosphonates); methyl and dimethylamine give monocondensation products thus permitting the synthesis of N-substituted aminoalkylphosphonates.
- Collignon, N.,Fabre, G.,Varlet, J. M.,Savignac, Ph.
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