摘要:
The present disclosure provides preparation method for water-soluble magnolol derivatives and honokiol derivatives and intermediates thereof, and related monohydroxy protection intermediates. The nitrification intermediate has a structure shown in Formula I. Formula I is
R 2 is a hydroxyl, and R 3 is H; or, R 2 is H, and R 3 is a hydroxyl; and R 1 and R 4 are independently selected from C 1 ~C 12 electron donor groups. The preparation method includes the following steps: performing monohydroxy protection on a compound A
with a hydroxy protection reagent in the presence of an acid binding agent to form a monohydroxy protection compound, herein R 1 , R 2 , R 3 and R 4 in the compound A have the same definition as above, and the hydroxy protection reagent is p-toluenesulfonyl chloride and 1-hydroxybenzotriazole; and performing a nitrification reaction and a deprotection reaction on the monohydroxy protection compound successively to obtain the nitrification intermediate. The present disclosure effectively improves the synthesis efficiency of the water-soluble magnolol derivative and honokiol derivative.
摘要:
A process for producing a labeled precursor which is useful for production of a radioactive fluorine-labeled amino acid compound is provided. In the reaction step for introducing a leaving group to a mixture of syn-form and anti-form of FACBC, a base is allowed to present in the reaction system to produce a syn-leaving group adduct which is unreactive with the base and is highly stable and an anti-leaving group adduct which can react with the base to form a water-soluble compound. By employing a purification method utilizing such a difference in solubility, the syn-leaving group adduct can be separated selectively. The base may be a linear-chain or branched-chain primary to tertiary alkylamine having 1 to 10 carbon atoms, a nitrogen-containing heterocyclic compound with 2 to 20 carbon atoms, and a nitrogen-containing hetero aromatic compound with 2 to 20 carbon atoms.