10-Methyl Docetaxel-D3 synthesis

Yield:1383561-32-7 0.52 g

Reaction Conditions:

with hydrogenchloride in ethanol at 0;Inert atmosphere;

Steps:

5 Synthesis of 1 0(3-(d3)-Methoxydocetaxel

The product was dissolved in 0.2N solution of hydrogen chloride in ethyl alcohol (40 ml) and stirred overnight at 00 C. under the nitrogen atmosphere. Next, the reaction mixture was diluted with distilled water (15 ml) and the product was extracted two times with dichloromethane (2x60 ml). The extract was dried (MgSO4) and concentrated to dryness under reduced pressure. The crude product was purifled by silica gel chromatography giving 0.52 g of the desired 1 0(3-(d3)-methoxydocetaxel.

References:

US2016/235705,2016,A1 Location in patent:Paragraph 0232; 0233