4 results about "Tryptophan methyl ester" patented technology

The invention discloses a preparation method and application of a compound with a cold sensing regulation effect, which comprises the following steps: dissolving tryptophan in methanol, adding concentrated sulfuric acid, esterifying the acid to protect carboxyl so as to obtain tryptophan methyl ester, dissolving the obtained tryptophan methyl ester and aromatic carboxylic acid substances in N, N-dimethylformamide, and reacting to obtain the compound with the cold sensing regulation effect. The method comprises the following steps: catalyzing 2-(7-azabenzotriazole)-N, N, N ', N'-tetramethylurea hexafluorophosphate and N, N-diisopropylethylamine, dissolving a catalyzed product in ethanol (98%), adding into a NaOH solution, stirring, carrying out rotary evaporation treatment, slowly dropwise adding a 0.5 mol / L hydrochloric acid solution, adjusting the pH value of a reaction system to 3-4, and finally obtaining the tryptophan derivative compound with the yield of 70%. The invention provides a potential medicine for improving the working ability and cold injury in the cold environment for people living and working in the cold environment, and is developed into a medicine for effectively improving neuropathic pain diseases in the cold environment.

The invention belongs to the technical field of medicines, and particularly relates to a beta-elemene tryptophan methyl ester derivative and application thereof in preparation of antitumor drugs. According to the beta-elemene tryptophan methyl ester derivative with the structure as shown in the formula (I), on the basis of maintaining a beta-elemene structural framework, a tryptophan methyl ester group is introduced to the 13th site of beta-elemene, and unsubstituted C3-7 heterocycloalkyl, substituted C3-7 heterocycloalkyl, unsubstituted C5-11 hetero-spirocycloalkyl or substituted C5-11 hetero-spirocycloalkyl is introduced to the 14th site of beta-elemene, so that the beta-elemene tryptophan methyl ester derivative with the structure as shown in the formula (I) is obtained. The water solubility and the pharmacokinetic property of the compound are effectively improved. Experimental results show that the anti-tumor activity of the beta-elemene tryptophan methyl ester derivative with the structure as shown in the formula (I) provided by the invention is obviously enhanced compared with that of beta-elemene. Formula (I).

The application relates to the technical field of organic synthesis, and discloses a method for preparing tadalafil or epi-tadalafil, which comprises the following steps: reacting N-(1,3-benzodioxol-5-methyl)-D-tryptophan methyl ester with Fomc-Ala-Cl to prepare compound IIa or compound IIb; and performing a deprotection / aminolysis reaction and a cyclization reaction on the compound IIa or the compound IIb in the presence of methylamine to prepare tadalafil or epi-tadalafil. Through the selection of a specific (Fomc-Ala-Cl) acylation reagent, the purity and / or yield of the compound IIa or the compound IIb are improved, so that the yield and / or purity of the tadalafil and / or epi-tadalafil are improved.

This invention discloses a method for preparing siliceous alkaloid A and its application. It belongs to the field of organic synthesis technology. This invention provides a method for synthesizing the compound siliceous alkaloid A, which employs a Pictet-Spengular reaction, causing L-tryptophan methyl ester hydrochloride to undergo a cyclization condensation reaction with methylglyoxal under acid catalysis, followed by ammonolysis to obtain the target compound. This method has the following advantages: simple reaction steps, eliminating the need for complex separation and purification, improving operational convenience; high reaction selectivity, yielding a high-purity target compound, improving synthesis efficiency; and low-cost reagents, reducing synthesis costs. This invention is the first to study the anti-anxiety activity of siliceous alkaloid A and elucidate its mechanism of action.