- Reaction of Imidazole and 2-Methylimidazole with Copper(II) Salts and Certain Acids
-
Abstract: Composition of biligand compounds Cu(C3H4N2, C4H6N2)x(Formula Presented.)2· nH2O obtained by reaction of aqueous suspensions of prepared poorly so
- Il’ina, K. A.,Kozik, V. V.,Skorik, N. A.
-
p. 1714 - 1721
(2021/11/24)
-
- Method for preparing folic acid by virtue of micro-channel reaction (by machine translation)
-
The invention belongs to the technical field of chemical synthesis of drugs, and relates to a synthesis method for preparing folic acid through a microchannel reactor. An intermediate 6 is prepared from cyanoethyl acetate as a raw material by one-step continuous operation, and the folic acid bulk drug is prepared through one-step reaction of the intermediate 6 and L - glutamate. The synthesis method uses the microchannel reactor to prepare the folic acid intermediate 2,triamino -4 - hydroxypyrimidine and folic acid, is safe and environment-friendly, and ensures the tasteless system. The method guarantees that the operation is simple and feasible, the solvent consumption is greatly reduced, 2,triamino -4 - hydroxyl pyrimidine yield and purity are obviously improved. (by machine translation)
- -
-
Paragraph 0058-0060
(2020/12/14)
-
- Preparation method of folic acid
-
The invention discloses a preparation method of folic acid. 2,4,5-triamino-6-hydroxypyrimidine hydrochloride is adopted as a reaction raw material, the compound has the great solubility in water, thusin the reaction process, the reaction area is increased, reaction selectivity is improved, a product is precipitated from a water solution, the obvious purification effect is achieved, and the yieldof a crude product reaches 90% or above; meanwhile, the using amount of a solvent, namely the water is remarkably lowered, compared with a traditional process, the water amount is lowered from 40-50 times to 5-10 times (relative to the mass ratio of N-(4-aminobenzoyl)-L-glutamic acid), and the yield is increased by 15-20%; and the yield of the synthesized folic acid is high, the product purity ishigh, reaction conditions are mild, the reaction speed is high, all the crude product water is reused, wastewater is less, safety and environmental friendliness are achieved, and thus the requirementof industrialization for environmental friendliness is met.
- -
-
Paragraph 0013-0014
(2019/05/08)
-
- Preparation method of 2,4,5-triamino-6-hydroxypyrimidine sulfate and folic acid
-
The invention relates to a preparation method of 2,4,5-triamino-6-hydroxypyrimidine sulfate and folic acid. The preparation method comprises the following steps: enabling cyanoacetate and sodium nitrite to be subjected to reaction under the action of an organic solvent and/or an inorganic solvent and an acidic substance to obtain 2-oximidocyanoacetate; then, enabling the 2-oximidocyanoacetate andguanidine hydrochloride to be subjected to reaction under an alkaline condition to obtain 2,4-diamino-5-isonitroso-6-oxopyrimidine; enabling the 2,4-diamino-5-isonitroso-6-oxopyrimidine and hydrogen gas to be subjected to reaction under an alkaline condition by means of action of Pd/C to obtain 2,4,5-triamino-6-hydroxypyrimidine, and adding sulfuric acid to adjust the pH value to obtain 2,4,5-triamino-6-hydroxypyrimidine sulfate; and then, adding trichloroacetone and N-(4-aminobenzoyl)-L-glutamic acid to be subjected to reaction in a buffer solution under the action of a catalyst molecular sieve so as to obtain the folic acid. Based on the process route, the invention explores the influences of different reaction steps and refining conditions on the preparation route of 2,4,5-triamino-6-hydroxypyrimidine sulfate and the folic acid so as to reduce the wastewater pollution while increasing the yield.
- -
-
Paragraph 0098-0121
(2019/04/10)
-
- Heteropolyacid catalyzed safe and green folic acid synthesis method
-
The invention belongs to the technical field of pharmaceutical chemistry synthesis, and relates to a heteropolyacid catalyzed safe and green folic acid synthesis method. The folic acid synthesis method comprises the following steps that (1), acrolein, heteropoly acid, 2,5,6-triamino-4-hydroxypyrimidine, p-aminobenzoate and alcoholic solvents are added into a reactor, stirring and warming are conducted, a reaction is conducted, material cooling is conducted after the reaction is finished, filtration is conducted, a filter cake is washed with the solvents, filtrate and washing liquid are combined, activated carbon is used for decoloration, the solvents are dried through distillation after extraction filtration is conducted, and a yellowish solid intermediate 6 is obtained; (2), sodium hydrogen glutamate and the intermediate 6 are dissolved into an alcohol-water mixed solution, stirring and a temperature reaction are conducted, after the reaction is finished, material cooling and coolingare conducted, heat preservation and crystallization are conducted, extraction filtration is conducted, the filter cake is washed with water, a crude folic acid product is obtained, and folic acid isobtained through refining. According to the synthesis method, acrolein which is low in price and easy to obtain is used as a raw material, the reaction is complete and rapid, no residue exists, it isguaranteed that the system is tasteless, and the yield and purity are obviously increased.
- -
-
Paragraph 0032; 0056; 0067-0075
(2019/10/01)
-
- Environment-friendly production method of folic acid
-
The invention provides a simple environment-friendly production method of folic acid. The method comprises the following steps: performing reaction of 2,4,5-triamino-6-hydroxypyrimidine sulfate, 1,1,3-trichloroacetone and N-p-aminobenzoyl-L-glutamic acid in a mixed solvent system of water and organic solvents to generate folic acid crude product, then refining by thionyl chloride in an organic solvent system to obtain a purified folic acid product, wherein the organic solvent used can be recycled by distillation. The purification method provided by the invention is simple in operation and lowin cost, and effectively reduces the generation of wastewater in folic acid production, and is suitable for requirements of industrialization to environmental protection.
- -
-
Paragraph 0032-0034; 0037
(2018/12/02)
-
- Preparation method of folic acid
-
The invention belongs to the technical field of medicine and particularly relates to a preparation method of folic acid, comprising the steps of (1) adding 1,1,3-tribromoacetone into ethanol solution, and stirring under heating; (2) dissolving the 1,1,3-tribromoacetone completely, continuing to add p-aminobenzoyl-L-glutamic acid, and stirring until full dissolution to obtain first reaction liquid; (3) dissolving 2,4,5-triamino-6-hydroxypyrimidine sulfate in water, and adjusting pH with saturated sodium carbonate until the 2,4,5-triamino-6-hydroxypyrimidine sulfate is fully dissolved to obtain second reaction liquid; (4) adding the second reaction liquid to the first reaction liquid, and allowing reacting under held temperature; (5) after reacting, performing suction filtering to obtain crude folic acid; (6) acid-dissolving the crude folic acid, alkali-dissolving, and refining to obtain finished folic acid. The preparation method of folic acid has the advantages that the defect that the prior art has high water consumption is changed from the purpose of saving resources and the integrated water saving is up to 40% and above.
- -
-
Paragraph 0025; 0026; 0027; 0028; 0029; 0030; 0031-0069
(2017/10/07)
-
- Folic acid preparation technology
-
The invention belongs to the technical field of medicine and chemical engineering, and particularly relates to a folic acid preparation technology. The technology comprises the steps of 1, dissolving 2,4-diamino-6-hydroxy-5-nitrosopyrimidine and nitrophenylcarbimide formylglutamicacid in water, adding NiAl2 to serve as a catalyst, and conducting hydrogenation reaction; 2, filtering a reaction solution obtained in step 1, taking filtrate, and recovering a NiAl2 catalyst obtained from filtration; 3, directly adding sodium metabisulfite into the filtrate, adding a trichloroacetone aqueous solution dropwise at 30-60 DEG C, and adding a sodium hydroxide solution to regulate pH; 4, conducting cooling crystallization and filter pressing on a solution obtained after reaction in step 3 to obtain a crude product, and refining the crude product to obtain pure folic acid. By the adoption of the technology, reaction efficiency is improved greatly, the preparing process is simplified, yield is increased, and generation of liquid waste and solid water is reduced greatly.
- -
-
Paragraph 0023; 0024; 0025; 0026; 0027; 0028; 0029-0031
(2017/06/20)
-
- New folic acid preparation method
-
The invention discloses a new folic acid preparation method, wherein folic acid is subjected to one-pot low temperature synthesis by using an ion liquid as a solvent. According to the present invention, the reaction condition is mild, the problems of more side reactions, high water consumption and complex refining process of the existing folic acid preparation method using the water as the solvent are solved, and the good foundation is established for the production capacity improving in the industrial production.
- -
-
Paragraph 0023; 0024; 0025; 0026; 0027; 0028; 0029-0046
(2017/03/17)
-
- Production method of folic acid
-
The invention relates to a production method folic acid. The production method sequentially includes following steps: synthesizing a crude product: using N-(p-aminobenzoyl)-L-glutamic acid shown as a compound A in a formula I, 2, 4, 5-triamino-6-hydroxy pyrimidine sulfate shown as a compound B in the formula I and trichloroacetone shown as a compound C in the formula I as raw material, sodium metabisulfite as an antioxidant and water as a solvent, and adopting a mode of charging in batches for graded cyclization reaction to obtain reaction liquid; subjecting the reaction liquid to cooling and press filtering to obtain a crude folic acid product; subjecting the crude folic acid product to acid dissolution, alkali dissolution and refining to obtain the folic acid. The mode of charging in batches is adopted to maintain concentration of materials in the reaction liquid within a reasonable range, so that water amount needed at the stage of synthesizing the crude folic acid product is reduced to 1/4 of that needed by existing synthesis processes.
- -
-
Paragraph 0012; 0035; 0046; 0047; 0056-0109
(2017/11/18)
-
- Environmentally friendly preparation method of synthetic folic acid
-
The invention relates to an environmentally friendly preparation method of synthetic folic acid. 2, 4, 5-triamino-6-hydroxypyrimidine sulfate, 1, 1, 2, 2, 3-pentachloropropane and N-P-aminobenzoyl-L-glutamic acid undergo a reaction to produce folic acid. Cheap and easily available 1, 1, 2, 2, 3-pentachloropropane replaces 1, 1, 3-trichloroacetone which is not easy to acquire and has low purity. The reaction process is simple and has characteristics of good regional selectivity, environmental friendliness, simple purification and low cost. The environmentally friendly preparation method has a good industrial production prospect.
- -
-
Paragraph 0017; 0018; 0019; 0020
(2017/08/28)
-
- Low-energy-consumption preparation method for synthesizing high-purity folic acid
-
The invention discloses a low-energy-consumption preparation method for synthesizing high-purity folic acid. The method comprises adding 2,4,5-triamino-6-hydroxypyrimidine sulfate, p-aminobenzamide glutamic acid, trichloroacetone, sodium acetate and sodium pyrosulfite into water, performing docking reaction, adjusting pH by adding solid sodium acetate before the reaction is started and separately adding a sodium hydroxide solution during reaction and after the reaction is finished, and filtering; performing acid-washing and filtering in hydrochloric acid solution; adding a magnesium oxide solution into water for reaction, adding active carbon for decoloring, and filtering; adjusting pH value by using hydrochloric acid, cooling and filtering; and washing with purified water and filtering, drying the filter cake, so as to obtain the final product. By using the method for producing folic acid, energy consumption is reduced, also yield and product purity are improved, and also cost is substantially saved.
- -
-
Paragraph 0029; 0030; 0031
(2016/10/08)
-
- Folic-acid cleaning production technology
-
The invention discloses a folic-acid cleaning production technology. The folic-acid cleaning production technology includes the steps that 2,4,5-triamino-6-hydroxy pyrimidine sulfate, p-amino benzamide glutamic acid and trichloroacetone are mixed and reacted under the condition that alkaline sodium hydroxide liquid exists, the reaction temperature ranges from 50 DEG C to 60 DEG C, pH ranges from 2.0 to 3.5, the reaction time ranges from 8 h to 10 h, and a crude product is obtained; sodium metabisulfite is added into the crude product and stirred for 0.5 h at the temperature of 38-40 DEG C, a sodium carbonate solution of 10% is added to keep pH ranging from 3 to 3.5 for 2 h, and first reaction liquid is obtained; the first reaction liquid is subjected to suction filtration, acid extracting, alkali refining and the like, and pure folic acid is prepared. By means of the folic-acid cleaning production technology, the yield of the prepared folic acid is 75% or above, and the purity is 95% or above.
- -
-
Paragraph 0033-0041
(2017/02/09)
-
- Folic acid synthesis method
-
The present invention relates to a folic acid synthesis method. According to the present invention, with the method, a 2,4,5-triamino-6-hydroxypyrimidine salt, 3-halogenated pyruvaldehyde oxime and N-(4-aminobenzamide)-L-glutamic acid are subjected to a reaction to prepare the folic acid; and the 3-halogenated pyruvaldehyde oxime is used to replace the low purity 1,1,3-trichloroacetone, such that the generation of a large amount of waste water in the traditional method is avoided, the reaction conditions are mild, the operation is easy, the reaction selectivity is good, the product purity is high, the advantages of safety and environmental protection are provided, and the method is suitable for the industrial requirements on environmental protection.
- -
-
Paragraph 0053; 0054
(2016/12/26)
-
- Oral B12 Therapy
-
Methods of normalizing vitamin B12 levels in patients with low vitamin B12 and methods of normalizing intersubject variability in the treatment of such patients are described. Methods of reducing MMA and/or homocysteine levels, and pharmaceutical compositions useful to effect such changes are also described.
- -
-
-
- DENDRIMER BASED MODULAR PLATFORMS
-
The present invention relates to novel therapeutic and diagnostic dendrimer based modular platforms (e.g., drug delivery platforms). In particular, the dendrimer based modular platforms are configured such that two or more dendrimers (e.g., PAMAM dendrimers) are coupled together (e.g., via a cycloaddition reaction) wherein each of the coupled dendrimers is functionalized (e.g., functionalized for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy). In some embodiments, the present invention provides dendrimer based modular platforms having coupled dendrimers (e.g., two or more coupled dendrimers) wherein each dendrimer is conjugated to one or more functional groups (e.g., therapeutic agent, imaging agent, targeting agent, triggering agent) (e.g., for specific targeting and/or therapeutic use of the dendrimer based modular platform). In some embodiments, the functional groups are conjugated to the dendrimers via a linker and/or a triggering agent. In addition, the present invention is directed to methods of synthesizing dendrimer based modular platforms, compositions comprising the dendrimer based modular platforms, as well as systems and methods utilizing the dendrimer based modular platforms (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, etc.)).
- -
-
-
- NUTRITIONAL FORMULATION
-
The present invention relates to nutritional supplements that provide an adult with essential vitamins and minerals that may be lacking in the adult's diet and prevent chronic diseases, such as osteoporosis. A number of combinations of nutrients in set ratios are provided to increase the body's ability to absorb and use the nutrients. These combinations are important in helping the body reach the proper balance required for maximized function. Because adults over the age of 50 years have different nutritional needs, nutritional supplements specifically designed for them are also provided.
- -
-
-
- Reaction between 7,8-dihydropterins and hydrogen peroxide under physiological conditions
-
In vitiligo, a common skin disorder that produces white patches of depigmentation, 7,8-dihydropterins accumulate in the presence of high concentration of H2O2. In this work, we present a study of the reaction between 7,8-dihydropterins and H2O2. The rate of the reaction, as well as the products formed, strongly depend on the chemical structure of the substituents. Electron-donor groups as substituents are the most reactive derivatives and undergo oxidation of the pterin moiety. The corresponding bimolecular rate constants at 37 °C in neutral aqueous solutions are reported. The biological implications of the results obtained are also discussed.
- Laura Dántola,Schuler, Tobias M.,Paula Denofrio,Vignoni, Mariana,Capparelli, Alberto L.,Lorente, Carolina,Thomas, Andrés H.
-
p. 8692 - 8699
(2008/12/21)
-
- Nutritional supplement
-
A nutritional supplement is provided that is designed to provide nutritional benefits as well as to assist the body with detoxification. By providing a supplement that serves both of these functions, the present invention may enable persons to improve their overall wellness.
- -
-
-
- Conjugates and compositions for cellular delivery
-
This invention features conjugates, degradable linkers, compositions, methods of synthesis, and applications thereof, including cholesterol, folate, galactose, galactosamine, N-acetyl galactosamine, PEG, phospholipid, peptide and human serum albumin (HSA) derived conjugates of biologically active compounds, including antibodies, antivirals, chemotherapeutics, peptides, proteins, hormones, nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids, DNAzymes, allozymes, antisense, dsRNA, siNA, siRNA, triplex oligonucleotides, 2,5-A chimeras, decoys and aptamers.
- -
-
-
- Vitamin/Mineral Compositions with DHA
-
Compositions containing the fatty acid docosahexaenoic acid (DHA) in combination with at least one vitamin and mineral are provided to supplement nutrition in a mammalian diet. DHA is present in the composition in concentrated amounts, advantageously in a carrier such as marinol oil, to allow for quantities of DHA sufficient to supply expectant and new mothers and their children as recommended on a daily basis. This DHA may also be used to treat a variety of disorders in children and adults. The compositions advantageously include vitamins, minerals, and optionally other nutrients to provide a nutritional supplement which may be convenient to swallow and taken once a day.
- -
-
-
- Conjugates and compositions for cellular delivery
-
This invention features conjugates, compositions, methods of synthesis, and applications thereof, including folate derived conjugates of nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids and antisense nucleic acid molecules.
- -
-
-
- Compositions and methods for prevention and treatment of chronic diseases and disorders including the complications of diabetes mellitus
-
This invention relates to nutrient and therapeutic compositions for treatment and prevention of symptoms and disease conditions associated with microangiopathy and macroangiopathy and to methods using the compositions. In particular, the invention relates to compositions useful in the treatment of diabetic retinopathy and nephropathy, to compositions useful in the treatment of other retinal disorders including macular degeneration and cataracts, to compositions useful in wound healing, to compositions useful for treatment and prevention of neuropathy, to compositions useful for treatment and prevention of cardiovascular disease and to compositions useful for the treatment and prevention of dental and periodontal disorders.
- -
-
-
- DNA encoding human κ casein and process for obtaining the protein
-
The present invention relates to an expression system comprising a DNA sequence encoding a polypeptide which has a biological activity of human κ-casein, the system comprising a 5′-flanking sequence capable of mediating expression of said DNA sequence. In preferred embodiments the 5′-flanking sequence is from a milk protein gene of a mammal such as a casein gene or whey acidic protein (WAP) gene and the DNA sequence contains at least one intron sequence selected from the intron sequences presented in SEQ ID NO:30. The invention also relates to DNA sequences, replicable expression vectors and cells harboring said vectors, recombinant polypeptide e.g. in glycosylated form, and milk, infant formula or nutrient supplement comprising recombinant polypeptide. The invention further relates to a transgenic non-human mammal such as a mouse, rat, rabbit, goat, sheep, pig, lama, camel or bovine species whose germ cells and somatic cells contain a DNA sequence as defined above as a result of chromosomal incorporation into the non-human mammalian genome, or into the genome of an ancestor of said non-human mammal.
- -
-
-
- Compounds for cardiovascular treatment comprising multi-vitamin and anti-platelet aggregating agents and methods for making and using the same
-
Compounds comprising multi-vitamins, zinc and an anti-platelet aggregating agent for the treatment of atherosclerotic cardiovascular disease (ASCVD) are disclosed. The compounds are provided in dosage form, and preferably include selected amounts of ascorbic acid, folic acid, vitamin E, vitamin B6 and vitamin B12. The anti-platelet aggregating agent preferably comprises aspirin. A protective coating is preferably provided between the aspirin and the other vitamin and mineral constituents. The dosages are effective in the treatment of ASCVD, and possess extended shelf lives.
- -
-
-
- Folic acid derivatives
-
Novel folic acid derivatives and their use in preparation of γ-esters of folic acid via a pteroyl azide intermediate are described. Folic acid γ-esters are useful intermediates in the synthesis of folic acid conjugates capable of binding folate receptors in vitro and in vivo.
- -
-
-
- Treatment and prevention of cardiovascular diseases with help of aspirin, antioxidants, niacin, and certain B vitamins
-
Disclosed is the method of reducing the incidence and severity of atherosclerosis, atherosclerotic central nervous system disease, claudication, coronary artery disease, homocystine related disorders, hypertension, peripheral vascular disease, presenile dementia and/or restenosis in humans by daily administration of an effective amount of a combination of acetylsalicylic acid (ASA), at least one antioxidant, a cyanocobalamin compound (Vitamin B12), a folic acid compound, a pyridoxine compound (Vitamin B6) and a niacin compound.
- -
-
-
- The synthesis of folic acid, multiply labelled with stable isotopes, for bio-availability studies in human nutrition
-
Two different methods for the synthesis of folic acid, which are suitable for the incorporation of compounds multiply labelled with stable isotopes, are described. The first method is based on the use of a novel reductive amination to link 2-acetyIamino-4-hydroxy-6-formylpteridine withp-aminobenzoyl-L-glutamic acid. The second method is based on the penultimate formation of an amide bond between Ar-2-acetyl-Ar-10-trifluoroacetyIpteroic acid and dimethyl L-glutamate. Both methods have been used to transform [13C6]aniline into folic acid, labelled with [13C6] in the p-aminobenzoate moiety, and [3,3,4,4-2H4]-L-glutamic acid into folic acid, labelled with [2H4] in the glutamate moiety. Doubly labelled [13C6,2H 4]-p-aminobenzoyl-L-glutamate has also been prepared by the former method.
- Maunder, Peter,Finglas, Paul M.,Mallet, Anthony I.,Mellon, Fred A.,Aaqib Razzaque,Ridge, Brian,Vahteristo, Liisa,Witthoeft, Cornelia
-
p. 1311 - 1323
(2007/10/03)
-
- Edible, low calorie compositions of a carrier and an active ingredient and methods for preparation thereof
-
Edible, low calorie compositions contain, in addition to an active ingredient, such as flavoring agents, sweetening agents, therapeutic agents, cosmetic agents and luminescent agents, a gel or glass carrier which is the amorphous reaction product of a basic amino acid, a carboxylic acid, a source of metallic ions and water. Methods of making the compositions are disclosed.
- -
-
-
- Folate-alp conjugate
-
Disclosed are novel folic acid-alkaline phosphatase conjugates useful in a competitive immunoassay for folic acid in a biological fluid such as serum. A preferred conjugate involves a folate hapten bound to (N-Succinimidyl?4-iodoacetyl!aminobenzoate) through a 1,12-diamino-4,9-dioxadodecanyl spacer arm.
- -
-
-
- Efficient syntheses of pyrofolic acid and pteroyl azide, reagents for the production of carboxyl-differentiated derivatives of folic acid
-
Reaction of folic acid (1) with excess trifluoroacetic anhydride provides access to both the previously unknown N10-(trifluoroacetyl)pyrrofolic acid (8) and pyrofolic acid (9). Reaction of either of these materials with hydrazine selectively affords pteroyl hydrazide (13), which may be oxidized to pteroyl azide (27) on a large scale (62% overall from I without the need for chromatography). Treatment of 27 with differentially protected glutamates provides a convenient and high-yielding synthesis of differentially protected, optically pure folates.
- Luo, Jin,Smith, Michael D.,Lantrip, Douglas A.,Wang, Susan,Fuchs
-
p. 10004 - 10013
(2007/10/03)
-
- Method for the production of folic acid
-
The present invention is directed to a novel process for the production of folic acid in high yield utilizing a novel diimine as an intermediate. This diimine is formed by reacting 2-substituted malondialdehyde with p-aminobenzoyl-L-glutamic acid. This diimine may be converted into folic acid by reacting said diimine with triaminopyrimidinone in the presence of sulphite.
- -
-
-
- Folinic acid-cyclodextrin inclusion compound
-
Complexes obtained by complexing folinic acid with α, β, γ, dimethyl-β or hydroxypropyl-β-cyclodextrin are described, having better activity in anemic syndromes due to folic acid deficiency than equivalent doses of the corresponding active principle. Furthermore the stability of said compounds in an acid environment renders them suitable to be administered by oral route.
- -
-
-
- Stabilized aqueous folic acid preparation
-
This invention relates to a stabilized aqueous folic acid preparation which comprises a folic acid component selected from the group consisting of folic acid, ammonium, alkali metal and alkaline earth metal salts of folic acid and mixtures thereof, and which has an improved stability of its folic acid contents in the presence of oxygen, the said preparation containing as a stabilizer a combination of (a) at least one member selected from the group consisting of dihydrofolic acid and ammonium, alkali metal, alkaline earth metal and alkanolammonium salts thereof, and (b) at least one member selected from the group consisting of at least one hydroxypolycarboxylic acid and ammonium, alkali metal, alkaline earth metal and alkanolammonium salts thereof.
- -
-
-
- Synthesis of 10-Propargylfolic Acid from 2-Amino-6-(bromomethyl)-4(1H)-pteridinone
-
6-(Bromomethyl)-2,4-pteridinediamine hydrobromide (1) is readily converted to 2-amino-6-(bromomethyl)-4(1H)-pteridinone hydrobromide (2) by treatment with 48percent hydrobromic acid.Compound 2 is of interest for direct attachment of the (2-amino-3,4-dihydro-4-oxo-6-pteridinyl)methyl group to appropriate side-chain precursors of analogues of folic acid, particularly those bearing functional groups incompatible with conditions required for hydrolytic deamination of the corresponding 2,4-diaminopteridine analogues.An example of the use of 2 in this connection is demonstrated through synthesis of 10-propargylfolic acid.
- Piper, James R.,McCaleb, George S.,Montgomery, John A.
-
p. 279 - 282
(2007/10/02)
-