JPWO2021097207A5

JPWO2021097207A5 -

Info

Publication number: JPWO2021097207A5
Application number: JP2022527117A
Authority: JP
Publication date: 2023-11-14

Claims

Formula 2A

A method for producing a compound having the structure

in the presence of hydrogen in a solvent with palladium.

1,2-dimethoxyethane (DME), K ₂ CO ₃ aqueous solution (3 eq.), Pd(PPh ₃ )Cl ₂ , 2-chloro-4-methylpyridin-3-amine, and 4,4,5,5 -Tetramethyl-2-(prop-1-en-2-yl)-1,3,2-dioxaborolane by reacting a mixture containing the structure:

2. The method of claim 1, comprising producing a compound having:

Formula 2A:

A method for preparing a compound of NaOH aqueous solution, structure:

and a mixture comprising sodium hypochlorite.

structure:

4. The method of claim 3, comprising preparing compound 36 by reacting compound ₃₅ having _H2SO4 .

structure:

By reacting compound 34 with DMF-DMA, NH ₄ OH and NH ₄ OOCCH ₃ , the structure:

5. The method of claim 4, comprising producing compound 35 having:

structure:

By reacting compound 33 with potassium tert-butoxide, ethyl isobutyrate, acetonitrile and L-proline, the structure:

6. The method of claim 5, comprising producing compound 34 having:

a. ) crotonaldehyde and (S)-α,α-bis[3,5-bis(trifluoromethyl)phenyl]-2-pyrrolidine methanol trimethylsilyl ether;
b. ) 4-methyl-3-oxopentanenitrile;
c. ) acetonitrile; and d. ) structure, including reacting hydroxylamine hydrochloride:

A method for producing compound 35 having

Using the compound of formula 2A above, formula 9:

2. The method of claim 1, which produces a compound having:

Using the compound of formula 2A above, formula 9:

4. The method of claim 3, which produces a compound having:

Using the compound of formula 2A above, formula 9:

8. The method of claim 7, which produces a compound having:

9. The method of claim 8, further comprising mixing the compound of Formula 9 with at least one pharmaceutically acceptable excipient to form a pharmaceutical composition.

10. The method of claim 9, further comprising mixing the compound of Formula 9 with at least one pharmaceutically acceptable excipient to form a pharmaceutical composition.

11. The method of claim 10, further comprising mixing the compound of Formula 9 with at least one pharmaceutically acceptable excipient to form a pharmaceutical composition.