- Process for preparing L-5 - methyl tetrahydrofolinate
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The invention relates to a preparation process of L-5 - methyl tetrahydrofolic acid, which adopts asymmetric catalytic hydrogenation to convert folic acid into (6S) - tetrahydro folic acid, and has high folic acid conversion rate, and (6S) - tetrahydrofolic acid diastereomeric excess degree. By salt formation and crystallization, the (6S) - tetrahydrofolic acid intermediate with extremely high diastereomeric excess can be easily enriched, and thus the yield and purity of L-5 - methyltetrahydrofolinate finally obtained are high. The catalytic hydrogenation process is very mature in industrial application and convenient to operate. The subsequent methylation and salt formation steps are easy to implement, and the preparation process has high economic value and practical value under the condition that the yield and purity of the product are improved.
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Paragraph 0050; 0053; 0055; 0057; 0058; 0060; 0061; 0063
(2021/11/06)
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- Preparation method of L-5-calcium methyltetrahydrofolate
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The invention discloses a preparation method of L-5-calcium methyltetrahydrofolate. The preparation method comprises the following steps of (1) adopting folic acid as a raw material, and reducing to preparing an intermediate 6-(R,S)-tetrahydrofolic acid; (2) carrying out chiral resolution on the 6-(R,S)-tetrahydrofolic acid, and obtaining an intermediate 6-S-tetrahydrofolate; (3) carrying out methylation on the 6-S-tetrahydrofolate to obtain an intermediate L-5-methyltetrahydrofolate; (4) reacting the L-5-methyltetrahydrofolate and salt containing calcium to obtain the L-5-calcium methyltetrahydrofolate. According to the method provided by the invention, the problem that hydrogen, wastewater and waste residues are easily generated by using a large number of sodium borohydride is avoided.
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Paragraph 0040; 0051; 0054; 0060; 0061
(2018/07/07)
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- Synthesis of (6S)-5,6,7,8-tetrahydrofolic acid
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A process for the large-scale chemoenzymatic production of (6S)-5-methyl-5,6,7,8-tetrahydrofolic acid, also known as (6S)-5-methylTHFA, the process comprising the steps of: (1) reducing folic acid (FA) so as to yield dihydrofolic acid (DHFA); (2) stereoselectively reducing DHFA with dihydrofolate reductase (DHFR) in the presence of NADP/NADPH, glucose and GluDH so as to yield (6S)-THFA; (3) converting (6S)-THFA to (6S)-5-methlTHFA; and (4) isolating (6S)-5-methylTHFA.
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Page/Page column
(2015/08/03)
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- RESOLUTION OF TETRAHYDROFOLIC ACID DERIVATIVES
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A process of preparing (6S)-tetrahydrofolic acid derivatives comprising reacting racemic (6RS)-tetrahydrofolic acid derivatives with N-alkyl-D-glucamine, forming N-alkyl-D-glucamine salts of the (6RS)-tetrahydrofolic acid derivatives, isolation of the N-alkyl-D-glucamine salt of the (6S)-tetrahydrofolic acid derivative, removal of the N-alkyl-D-glucamine cation and purification of the (6S)-tetrahydrofolic acid derivative. The purified (6S)-tetrahydrofolic acid derivative can then be converted into the corresponding alkali metal or alkaline earth metal salts.
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- A PROCESS FOR THE PREPARATION OF THE STABLE, AMORPHOUS CALCIUM SALT OF (6S)-N(5)-METHYL-5,6,7,8-TETRAHYDROFOLIC ACID
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A process for the preparation of an aqueous solution of the calcium salt of (6S)-N(5)-methyl-5,6,7,8-tetrahydrofolic acid, whereby (6S)-5,6,7,8-tetrahydrofolic acid having a content of the corresponding (6R)-diastereoisomer in the range from 4% by weight to 8% by weight is methylated in water comprises: treating the methylated reaction mixture with calcium chloride; crystallizing the calcium salt of (6RS)-N(5)-methyl-5,6,7,8-tetrahydrofolic acid from the resulting aqueous solution; and obtaining an aqueous solution of the calcium salt of (6S)-N(5)-methyl-5,6,7,8-tetrahydrofolic acid.
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Page/Page column 3
(2010/07/08)
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