Cyclotheonellazolea, and synthetic method therefor, and application method thereof

A synthetic method of a CyclotheonellazoleA, comprising:

• removing a 9-fluorenylmethyloxycarbonyl (Fmoc) protection group from a compound 2 with diethylamine (DEA) to obtain a first group-removed compound, and performing a peptide grafting reaction on the first group-removed compound and a compound 30 to obtain a compound 31;
• and removing a t-butyloxy carbonyl (Boc) protection group from the compound 31 with trifluoroacetic acid (TFA) to obtain a second group-removed compound, and performing a peptide grafting reaction on the second group-removed compound and a compound 32 to obtain a compound 33;
• wherein a specific synthesis process of the compound 33 is as follows:
• ;
• removing a tert-butyldiphenylsilyl (TBDPS) protection group from the compound 33 with ammonium fluoride (NH4F) to obtain a third group-removed compound, and activating a hydroxyl group of the third group-removed compound with methanesulfonyl chloride (MsCl) to obtain activated compound;
• performing a bimolecular nucleophilic substitution (SN2) reaction on the activated compound with potassium thioacetate (KSAc) to obtain a thioester;
• oxidizing the thioester with potassium monopersulphate triple salt (Oxone) to obtain a first sulfurous acid;
• removing a pivaloyl (Piv) group from the first sulfurous acid with triethylamine (C6H15N) in a reflux condition of methanol (MeOH) to obtain a secondary alcohol;
• oxidizing the secondary alcohol with 2-iodoxybenzoic acid (IBX) to obtain a α-ketoamide;
• and oxidizing the α-ketoamide with selenium dioxide (SeO2) to remove two allyl groups from the α-ketoamide, to thereby obtain a second sulfurous acid, and adding a saturated sodium chloride solution into the second sulfurous acid to obtain the CyclotheonellazoleA;
• wherein a specific synthesis process of the CyclotheonellazoleA is as follows:
• and
• wherein structures of the compound 2, the compound 30 and the compound 33 are as follows:
• ;
• ;
• .