154-87-0

Usage

Uses

Used in Pharmaceutical Industry:
Cocarboxylase is used as a certified pharmaceutical secondary standard for quality control, providing a convenient and cost-effective alternative to in-house working standards for pharmaceutical laboratories and manufacturers.
Used in Biochemical Reactions:
Cocarboxylase is used as a cofactor to catalyze various biochemical reactions, particularly in the cleavage of ribulose-5-phosphate by transketolase, forming D-glyceraldehyde-3-phosphate. This reaction requires the addition of an acceptor aldehyde such as ribose-5-phosphate, glyceraldehyde, or glycolaldehyde.
Used in Decarboxylation Mechanisms:
Cocarboxylase is utilized in decarboxylation mechanisms in biological systems, aiding in the investigation of radical reactions of thiamin pyrophosphate in 2-oxoacid oxidoreductases.

Originator

Actimide,Tobishi

Manufacturing Process

4.5 kg of aqueous 89% orthophosphoric acid are heated to 135°C, and kept at this temperature for about 3 h while being actively stirred. Then, the heating is discontinued and 3.5 kg of phosphorouspentoxide are added during a period of 2.5 to 3 h, while being actively stirred. During this period, the interior temperature rises to 165°-175°C. After completion of the addition of phosphorouspentoxide, the stirring is continued until all phosphorouspentoxide is dissolved. The phosphoric acid mixture thus produced is subsequently cooled down to 130°C. At this temperature 2.0 kg of thiamine chloride hydrochloride (vitamin B1) were added during 2 to 3 h while being well stirred. The stirring is continued at 130°C until the phosphorylated mixture no longer contains chlorine ions. A phosphorylated melt is thus obtained. The thus obtained phosphorylation melt is dissolved in 6-8 L of water (with ice) at a temperature below 10°C, while being vigorously stirred. The aqueous solution is stirred into 100 L of 96% alcohol and left standing overnight. The supernatant solvent is decanted from the separated syrup; the latter is taken up in 4 L of water. The solution thus obtained is fed, depending upon the volume of phosphoric acid contained therein, to an exchanger column filled with anion exchanger (weak basic, for instance Amberlite IRA 45, 20-30 L) (a polystyrene resin with primary, secondary and quaternary amino groups). The solution is caused to seep into the column from the top thereof and is then washed with water until the runoff at the bottom no longer shows any thiamine reaction. About 25 L of the solution are obtained, which are concentrated to 6 L at 30°C and 12 Torr. The concentrated residue is added to 20 to 30 L of a cationic exchanger (Amberlite IRC 50) in order to separate the thiamine-orthophosphoric acid ester from the thiamine-pyrophosphoric acid ester, and subsequently washed with water until the eluate is free of thiamine. 70-80 L of a solution are obtained which are concentrated to 1.5 L in a circulation evaporator at 30°C and 12 Torr. 7.5 L of 96% ethanol are slowly added to a concentrate while being stirred. The cocarboxylase-tetrahydrate separates in the form of fine needles. The yield is 530.0 g with a melting point of 220°-225°C (dec.). 10.0 g of cocarboxylase-tetrahydrate are dissolved in 25 ml of 5% aqueous hydrochloric acid, and 75 ml acetone are added dropwise while being stirred. The precipitated hydrochloride of the cocarboxylase, melting point 240°C is sucked off. The yield is 9.5 g.

Therapeutic Function

Coenzyme, Metabolic

Biochem/physiol Actions

Thiamine pyrophosphate (TPP) is a coenzyme of transketolase, that catalyzes the cleavage of ribulose-5-phosphate. This reaction leads to the formation of D-glyceraldehyde-3-phosphate. It requires the addition of an acceptor aldehyde such as ribose-5-phosphate, glyceraldehye or glycolaldehyde. TPP is capable of decarboxylating hydroxypyruvate in the presence of an ′acceptor aldehyde′.

InChI:InChI=1/C12H18N4O7P2S.ClH/c1-8-11(3-4-22-25(20,21)23-24(17,18)19)26-7-16(8)6-10-5-14-9(2)15-12(10)13;/h5,7H,3-4,6H2,1-2H3,(H4-,13,14,15,17,18,19,20,21);1H

Synthetic route

thiamin triphosphate (50851-39-3) + Thiamine hydrochloride (67-03-8) → thiamine diphosphate (154-87-0) + 2-[3-[(4-amino-2-methylpyrimidin-5-yl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethyl dihydrogen phosphate (10023-48-0)

Conditions	Yield
With meta-phosphoric acid

4-methyl-5-oxyethyl thiazol diphosphate (2606-90-8) + 4-amino-5-bromomethyl-2-methylpyrimidine hydrobromide (2908-71-6) → thiamine diphosphate (154-87-0)

Conditions	Yield
(i) , (ii) ion exchange resin (H+-form); Multistep reaction;

diphosphoric acid 1,1-dibenzyl ester 2-[2-(4-methyl-thiazol-5-yl)-ethyl] ester; cyclohexylamine salt (4066-53-9) → thiamine diphosphate (154-87-0)

Conditions	Yield
Multi-step reaction with 2 steps 1: (i) ion exchange resin +-form>, (ii) H2, PdCl2, MeOH, (iii) ion exchange resin --form> 2: (i) , (ii) ion exchange resin (H+-form) View Scheme

Thiamine hydrochloride (67-03-8) → thiamine monophosphate chloride (532-40-1) + thiamine diphosphate (154-87-0)

Conditions	Yield
With sodium pyrophosphate at 120℃;

vitamin B1 (59-43-8) → thiamine diphosphate (154-87-0)

Conditions	Yield
With thiamin pyrophosphokinase; ATP; magnesium chloride In aq. buffer at 37℃; for 2h; pH=8; Inert atmosphere; Enzymatic reaction;

5-(3-acetoxyphenyl)-4-(13-carboxy-1,1-dimethyl-3-oxatridecan-1-yl)-3,3-dimethyl-2,3-dihydrofuran (594859-88-8) + thiamine diphosphate (154-87-0) → 1-(3-acetoxyphenyl)-5-(13-carboxy-1,1-dimethyl-3-oxatridecan-1-yl)-4,4-dimethyl-2,6,7-trioxabicyclo[3.2.0]heptane (594859-89-9)

Conditions	Yield
In hexane; dichloromethane; ethyl acetate	97.6%

5-(3-t-butyldimethylsiloxyphenyl)-3,3-dimethyl-4-(1,1-dimethyl-13-succinimidoxycarbonyl-3-oxatridecan-1-yl)-2,3-dihydrofuran + thiamine diphosphate (154-87-0) → 1-(3-t-butyldimethylsiloxyphenyl)-4,4-dimethyl-5-(1,1-dimethyl-13-succinimidoxycarbonyl-3-oxatridecan-1-yl)-2,6,7-trioxabicyclo[3.2.0]heptane

Conditions	Yield
In hexane; dichloromethane; ethyl acetate	97.5%

5-(3-t-butyldimethylsiloxyphenyl)-3,3-dimethyl-4-(1,1-dimethyl-7-succinimidoxycarbonyl-3-oxaheptyl)-2,3-dihydrofuran + thiamine diphosphate (154-87-0) → 1-(3-t-butyldimethylsiloxyphenyl)-4,4-dimethyl-5-(1,1-dimethyl-7-succinimidoxycarbonyl-3-oxaheptyl)-2,6,7-trioxabicyclo[3.2.0]heptane

Conditions	Yield
In hexane; dichloromethane; ethyl acetate	83.6%

5-(3-acetoxyphenyl)-3,3-dimethyl-4-(1,1-dimethyl-13-succinimidoxycarbonyl-3-oxatridecan-1-yl)-2,3-dihydrofuran + thiamine diphosphate (154-87-0) → 1-(3-acetoxyphenyl)-4,4-dimethyl-5-(1,1-dimethyl-13-succinimidoxycarbonyl-3-oxatridecan-1-yl)-2,6,7-trioxabicyclo[3.2.0]heptane

Conditions	Yield
In hexane; dichloromethane; ethyl acetate	82.5%

5-(3-acetoxyphenyl)-4-(13-ethoxycarbonyl-1,1-dimethyl-3-oxatridecan-1-yl)-3,3-dimethyl-2,3-dihydrofuran (594859-90-2) + thiamine diphosphate (154-87-0) → 1-(3-acetoxyphenyl)-5-(13-ethoxycarbonyl-1,1-dimethyl-3-oxatridecan-1-yl)-4,4-dimethyl-2,6,7-trioxabicyclo[3.2.0]heptane (594859-91-3)

Conditions	Yield
In hexane; dichloromethane; ethyl acetate	75%

bis(acetylacetonate)oxovanadium (3153-26-2) + water (7732-18-5) + thiamine diphosphate (154-87-0) + N,N-dimethyl-formamide (68-12-2, 33513-42-7) → PV14O42(9-)*3C2H7N*3H(1+)*2C12H17N4O4PS*6H3O(1+)

Conditions	Yield
With nitric acid at 20 - 100℃; for 75h; pH=3; Sealed tube; High pressure;	73%

octane-2,3-dione (585-25-1) + thiamine diphosphate (154-87-0) → (3S)-3-hydroxy-3-methylnonane-2,4-dione (1421833-45-5) + 3-hydroxy-3-pentylpentane-2,4-dione (1421833-43-3)

Conditions	Yield
With ethylenediaminetetraacetic acid; acetylacetoin synthase; magnesium sulfate In aq. phosphate buffer at 30 - 80℃; for 20.3333h; pH=6.5; Enzymatic reaction;	A 68% B 30%

thiamine diphosphate (154-87-0) → thiamine monophosphate chloride (532-40-1)

Conditions	Yield
With sulfuric acid

thiamine diphosphate (154-87-0) → 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; iodide

Conditions	Yield
With sulfuric acid

thiamine diphosphate (154-87-0) → 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; dihydrogenphosphate

Conditions	Yield
With sulfuric acid

thiamine diphosphate (154-87-0) → 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; fluoride-dihydro fluoride

Conditions	Yield
With sulfuric acid

thiamin triphosphate (50851-39-3) + Thiamine hydrochloride (67-03-8) → thiamine diphosphate (154-87-0) + 2-[3-[(4-amino-2-methylpyrimidin-5-yl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethyl dihydrogen phosphate (10023-48-0)

Conditions	Yield
With meta-phosphoric acid

4-methyl-5-oxyethyl thiazol diphosphate (2606-90-8) + 4-amino-5-bromomethyl-2-methylpyrimidine hydrobromide (2908-71-6) → thiamine diphosphate (154-87-0)

Conditions	Yield
(i) , (ii) ion exchange resin (H+-form); Multistep reaction;

diphosphoric acid 1,1-dibenzyl ester 2-[2-(4-methyl-thiazol-5-yl)-ethyl] ester; cyclohexylamine salt (4066-53-9) → thiamine diphosphate (154-87-0)

Conditions	Yield
Multi-step reaction with 2 steps 1: (i) ion exchange resin +-form>, (ii) H2, PdCl2, MeOH, (iii) ion exchange resin --form> 2: (i) , (ii) ion exchange resin (H+-form) View Scheme

Thiamine hydrochloride (67-03-8) → thiamine monophosphate chloride (532-40-1) + thiamine diphosphate (154-87-0)

Conditions	Yield
With sodium pyrophosphate at 120℃;

vitamin B1 (59-43-8) → thiamine diphosphate (154-87-0)

Conditions	Yield
With thiamin pyrophosphokinase; ATP; magnesium chloride In aq. buffer at 37℃; for 2h; pH=8; Inert atmosphere; Enzymatic reaction;

5-(3-acetoxyphenyl)-4-(13-carboxy-1,1-dimethyl-3-oxatridecan-1-yl)-3,3-dimethyl-2,3-dihydrofuran (594859-88-8) + thiamine diphosphate (154-87-0) → 1-(3-acetoxyphenyl)-5-(13-carboxy-1,1-dimethyl-3-oxatridecan-1-yl)-4,4-dimethyl-2,6,7-trioxabicyclo[3.2.0]heptane (594859-89-9)

Conditions	Yield
In hexane; dichloromethane; ethyl acetate	97.6%

5-(3-t-butyldimethylsiloxyphenyl)-3,3-dimethyl-4-(1,1-dimethyl-13-succinimidoxycarbonyl-3-oxatridecan-1-yl)-2,3-dihydrofuran + thiamine diphosphate (154-87-0) → 1-(3-t-butyldimethylsiloxyphenyl)-4,4-dimethyl-5-(1,1-dimethyl-13-succinimidoxycarbonyl-3-oxatridecan-1-yl)-2,6,7-trioxabicyclo[3.2.0]heptane

Conditions	Yield
In hexane; dichloromethane; ethyl acetate	97.5%

5-(3-t-butyldimethylsiloxyphenyl)-3,3-dimethyl-4-(1,1-dimethyl-7-succinimidoxycarbonyl-3-oxaheptyl)-2,3-dihydrofuran + thiamine diphosphate (154-87-0) → 1-(3-t-butyldimethylsiloxyphenyl)-4,4-dimethyl-5-(1,1-dimethyl-7-succinimidoxycarbonyl-3-oxaheptyl)-2,6,7-trioxabicyclo[3.2.0]heptane

Conditions	Yield
In hexane; dichloromethane; ethyl acetate	83.6%

5-(3-acetoxyphenyl)-3,3-dimethyl-4-(1,1-dimethyl-13-succinimidoxycarbonyl-3-oxatridecan-1-yl)-2,3-dihydrofuran + thiamine diphosphate (154-87-0) → 1-(3-acetoxyphenyl)-4,4-dimethyl-5-(1,1-dimethyl-13-succinimidoxycarbonyl-3-oxatridecan-1-yl)-2,6,7-trioxabicyclo[3.2.0]heptane

Conditions	Yield
In hexane; dichloromethane; ethyl acetate	82.5%

5-(3-acetoxyphenyl)-4-(13-ethoxycarbonyl-1,1-dimethyl-3-oxatridecan-1-yl)-3,3-dimethyl-2,3-dihydrofuran (594859-90-2) + thiamine diphosphate (154-87-0) → 1-(3-acetoxyphenyl)-5-(13-ethoxycarbonyl-1,1-dimethyl-3-oxatridecan-1-yl)-4,4-dimethyl-2,6,7-trioxabicyclo[3.2.0]heptane (594859-91-3)

Conditions	Yield
In hexane; dichloromethane; ethyl acetate	75%

bis(acetylacetonate)oxovanadium (3153-26-2) + water (7732-18-5) + thiamine diphosphate (154-87-0) + N,N-dimethyl-formamide (68-12-2, 33513-42-7) → PV14O42(9-)*3C2H7N*3H(1+)*2C12H17N4O4PS*6H3O(1+)

Conditions	Yield
With nitric acid at 20 - 100℃; for 75h; pH=3; Sealed tube; High pressure;	73%

octane-2,3-dione (585-25-1) + thiamine diphosphate (154-87-0) → (3S)-3-hydroxy-3-methylnonane-2,4-dione (1421833-45-5) + 3-hydroxy-3-pentylpentane-2,4-dione (1421833-43-3)

Conditions	Yield
With ethylenediaminetetraacetic acid; acetylacetoin synthase; magnesium sulfate In aq. phosphate buffer at 30 - 80℃; for 20.3333h; pH=6.5; Enzymatic reaction;	A 68% B 30%

thiamine diphosphate (154-87-0) → thiamine monophosphate chloride (532-40-1)

Conditions	Yield
With sulfuric acid

thiamine diphosphate (154-87-0) → 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; iodide

Conditions	Yield
With sulfuric acid

thiamine diphosphate (154-87-0) → 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; dihydrogenphosphate

Conditions	Yield
With sulfuric acid

thiamine diphosphate (154-87-0) → 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; fluoride-dihydro fluoride

Conditions	Yield
With sulfuric acid

thiamine diphosphate (154-87-0) → 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; hydrochloride (129681-12-5)

Conditions	Yield
With sulfuric acid

thiamine diphosphate (154-87-0) → 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; bromide hydrobromide

Conditions	Yield
With sulfuric acid

thiamine diphosphate (154-87-0) → 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; nitrate

Conditions	Yield
With sulfuric acid

thiamine diphosphate (154-87-0) → 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; perchlorate

Conditions	Yield
With sulfuric acid

thiamine diphosphate (154-87-0) → 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; hydrogen sulfate

Conditions	Yield
With sulfuric acid

thiamine diphosphate (154-87-0) → 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; naphthalene-2-sulfonate

Conditions	Yield
With sulfuric acid

thiamine diphosphate (154-87-0) → 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; bis phosphate

Conditions	Yield
With sulfuric acid

thiamine diphosphate (154-87-0) → 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; disulfate

Conditions	Yield
With sulfuric acid

t-butyl pyruvate (76849-54-2) + thiamine diphosphate (154-87-0) → C19H31N4O10P2S(1+)*Cl(1-) (76849-52-0)

Conditions	Yield
With tetra(n-butyl)ammonium hydroxide; sodium t-butanolate 1) water; 2) DMF, -5 deg C, 30 min; Multistep reaction;

formaldehyd (50-00-0) + thiamine diphosphate (154-87-0) → 2-Hydroxymethylthiamine diphosphate

Conditions	Yield
With sodium hydroxide In various solvent(s) at 20℃; for 24h; pH=5.6; Addition;

Upstream product

• 50851-39-3 thiamin triphosphate 
• 67-03-8 Thiamine hydrochloride 
• 2606-90-8 4-methyl-5-oxyethyl thiazol diphosphate 
• 2908-71-6 4-amino-5-bromomethyl-2-methylpyrimidine hydrobromide 
• 4066-53-9 diphosphoric acid 1,1-dibenzyl ester 2-[2-(4-methyl-thiazol-5-yl)-ethyl] ester; cyclohexylamine salt 
• 59-43-8 vitamin B₁ 
• 136-09-4 thiamine pyrophosphate 

Downstream Products

• 532-40-1 thiamine monophosphate chloride 
• 129681-12-5 3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-4-methyl-5-(2-phosphonooxy-ethyl)-thiazolium; hydrochloride 
• 594859-82-2 1-(3-acetoxyphenyl)-5-(7-carboxy-1,1-dimethyl-3-oxaheptyl)-4,4-dimethyl-2,6,7-trioxabicyclo[3.2.0]heptane 
• 594859-84-4 1-(3-acetoxyphenyl)-5-(7-ethoxycarbonyl-1,1-dimethyl-3-oxaheptyl)-4,4-dimethyl-2,6,7-trioxabicyclo[3.2.0]heptane 
• 594859-89-9 1-(3-acetoxyphenyl)-5-(13-carboxy-1,1-dimethyl-3-oxatridecan-1-yl)-4,4-dimethyl-2,6,7-trioxabicyclo[3.2.0]heptane 
• 594859-91-3 1-(3-acetoxyphenyl)-5-(13-ethoxycarbonyl-1,1-dimethyl-3-oxatridecan-1-yl)-4,4-dimethyl-2,6,7-trioxabicyclo[3.2.0]heptane 
• 216229-01-5 (2R,3S)-1-Boc-2-t-butyldimethylsilyloxymethyl-3-benzoyloxypyrrolidine 
• 158175-22-5 4'-(Octadecyloxy)-5-nonyl-2-phenylpyrimidine 
• 192449-21-1 5-isopropyl-1-(3-methoxy)phenyl-2,6,7-trioxabicyclo[3.2.0]heptane 
• 190516-26-8 5-isopropyl-1-(3-methoxy)phenyl-4,4-dimethyl-2,6,7-trioxabicyclo[3.2.0]heptane 
• 190516-34-8 1(3-t-butyldimethylsiloxy)phenyl-5-isopropyl-4,4-dimethyl-2,6,7-trioxabicyclo[3.2.0]heptane 
• 59-43-8 vitamin B₁ 
• 213381-59-0 2-methyl-7-(3,5-bis(trifluoromethyl)phenyl)-1-indanone 

Related news

Application of Microwave Irradiation for Concentrating of the Cocarboxylase (cas 154-87-0) Water Solutions09/30/2019

A process for concentrating of cocarboxylase water solutions under microwave irradiation is investigated. Perspectives of application of microwave technology for evaporating of the water solutions are showndetailed

Effects of Cocarboxylase (cas 154-87-0) in Amikacin-Induced Ototoxicity in Immature Animals09/29/2019

Possible otoprotective properties of cocarboxylase were studied on the model of amikacin-induced ototoxicity in immature rabbits. Auditory function was evaluated by the short-latency auditory brainstem response (ABR) and distortion product otoacoustic emission (DPOAE) tests. Administration of co...detailed

Influence of microwave technology on Cocarboxylase (cas 154-87-0) hydrochloride particle diversity and drying efficiency09/28/2019

Two possible ways of crystallite downsizing of cocarboxylase hydrochloride namely mechanical milling and precipitation under high supersaturation conditions were studied as well as their influence on the drying parameters of the produced powders. It was found that both methods allowed shortening...detailed

Relevant academic research and scientific papers

Synthesis and characterization of catalytically active thiazolium gold(i)-carbenes

Thiamin analogs were used to synthesize mono gold(i)-carbene derivatives in a single step under aqueous conditions. The resulting thiazolium gold(i)-carbenes catalyze 5-endo-dig carbocyclization of an acetylenic dicarbonyl compound in organic solvents and hydroalkoxylation of an allene in aqueous buffer.

Product inhibition of mammalian thiamine pyrophosphokinase is an important mechanism for maintaining thiamine diphosphate homeostasis

Background: Thiamine diphosphate (ThDP), an indispensable cofactor for oxidative energy metabolism, is synthesized through the reaction thiamine + ATP ? ThDP + AMP, catalyzed by thiamine pyrophosphokinase 1 (TPK1), a cytosolic dimeric enzyme. It was claimed that the equilibrium of the reaction is in favor of the formation of thiamine and ATP, at odds with thermodynamic calculations. Here we show that this discrepancy is due to feedback inhibition by the product ThDP. Methods: We used a purified recombinant mouse TPK1 to study reaction kinetics in the forward (physiological) and for the first time also in the reverse direction. Results: Keq values reported previously are strongly underestimated, due to the fact the reaction in the forward direction rapidly slows down and reaches a pseudo-equilibrium as ThDP accumulates. We found that ThDP is a potent non-competitive inhibitor (Ki ≈ 0.4 μM) of the forward reaction. In the reverse direction, a true equilibrium is reached with a Keq of about 2 × 10?5, strongly in favor of ThDP formation. In the reverse direction, we found a very low Km for ThDP (0.05 μM), in agreement with a tight binding of ThDP to the enzyme. General significance: Inhibition of TPK1 by ThDP explains why intracellular ThDP levels remain low after administration of even very high doses of thiamine. Understanding the consequences of this feedback inhibition is essential for developing reliable methods for measuring TPK activity in tissue extracts and for optimizing the therapeutic use of thiamine and its prodrugs with higher bioavailability under pathological conditions.

Preparation method of co-carboxylase and tetrahydrate or salt thereof

The invention discloses a preparation method of co-carboxylase and tetrahydrate or salt thereof. The invention provides a preparation method of a co-carboxylase shown as a formula I. The method comprises the following steps: eluting a mixture containing the co-carboxylase as shown in the formula I by using weakly-alkaline anion exchange resin through water and a weakly-alkaline aqueous solution with the pH value of 10-12 as eluent in sequence, and collecting eluate to obtain an aqueous solution containing the co-carboxylase as shown in the formula I, wherein the mixture containing the co-carboxylase as shown in the formula I comprises thiamine monophosphate and the co-carboxylase as shown in the formula I.

A PROCESS FOR THE PREPARATION OF A THIAMINE DERIVATIVE AND SALT THEREOF

A process for the preparation of a thiamine derivative and salt thereof, the process comprising the steps of: reacting thiamine chloride hydrochloride with phosphoric acid in the presence of a catalyst to produce a reaction mass of thiamine polyphosphates; isolating said thiamine derivative from said reaction mass of thiamine polyphosphates; and preparing salt of said thiamine derivative.

Use of vitamin b1 as agents for controlling plant diseases

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Method for treating fibrotic diseases or other indications IC

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Process for producing 1,4-dihydroxy-2-arylnaphthoate

Pure 1,4-dihydroxy-2-arylnaphthoate is prepared in high yield by allowing 1,4-dihydroxy-2-naphthoic acid to react with triarylphosphite in the presence of an acid catalyst selected from organic and inorganic acids and crystallizing from a mixed solvent consisting essentially of lower alcohols and water until 1,4-dihydroxy-2-naphthoic acid is isolated and is further purified by crystallization from a mixed solvent consisting essentially of lower alcohols, water and extraction solvent, i.e., alkyl-substituted aromatic hydrocarbons or halogen-substituted aliphatic or aromatic hydrocarbons.

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Process for preparing tertiary phosphines

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