Endomorphin analog modified by hydroxylation of 4-phenylpropanamide and its synthesis method and application
A technology of phenylpropanamide hydroxyl and endomorphin, applied in the direction of drug combination, tetrapeptide composition, peptide/protein composition, etc., can solve blood pressure reduction, cardiovascular system side effects, affinity, opioid agonist activity, and analgesia Features need to be improved
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specific Embodiment approach 1
[0076] Specific embodiment 1: The endomorphin analogue modified by the hydroxylation of the 4-phenylpropanamide in this embodiment is an endomorphin-1 analogue, tyrosine-proline-tryptophan-phenylpropanoid (N-hydroxyl) Amide, its structure is as follows:
[0077]
specific Embodiment approach 2
[0078] Specific embodiment two: the synthesis method of endomorphin analogs modified by hydroxylation of 4-phenylpropanamide in the present embodiment comprises the following steps:
[0079] One, the synthesis of N-tert-butoxycarbonyl-phenylpropanoid (N-hydroxyl) amide
[0080] Add N-tert-butoxycarbonyl-phenylalanine and N-hydroxysuccinimide into redistilled tetrahydrofuran, stir at 0-5°C to obtain reaction solution A; wherein N-tert-butoxycarbonyl-phenylalanine The molar ratio of N-hydroxysuccinimide is 1:1.2~1.4;
[0081] Dissolve N,N'-dicyclohexylcarbodiimide in tetrahydrofuran, add it to reaction solution A, stir and react at 0-5°C for 20-40 minutes, and then react at room temperature for 4-8 hours; where N-tert-butoxycarbonyl- The molar ratio of phenylalanine to N,N'-dicyclohexylcarbodiimide is 1:1.2~1.4;
[0082] Filter out the product 1,3-dicyclohexyl urea, retain the activated ester filtrate, dissolve hydroxylamine hydrochloride in water, adjust the pH value to 9-11,...
specific Embodiment approach 3
[0103] Specific embodiment three: the difference between this embodiment and specific embodiment two is: the washing method in step one is: wash with 5% citric acid solution, saturated sodium bicarbonate solution and saturated sodium chloride solution successively. Others are the same as in the second embodiment.
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