Back to results
US 2023/0068240 A1Published application
A Process for the Steroselective Preparation of Chiral 2-[(Hetero)Arylalkylsulfanyl]Pyrimidines and Products Obtainable Therefrom
AssigneeKancera AB
InventorsJan Vågberg, Styrbjörn Byström
Life of this patent
Estimating the term…
Abstract
Described herein is a process for the preparation of a compound of Formula I, wherein R1 and R2 each have the meanings provided in the description. Also described is a process for the preparation of pharmaceutically-active compounds including the process for the preparation of compounds of Formula I.
Claims19
1-32. (canceled)
A compound 2-[(2-amino-5-[(1-phenylethyl)thio][1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-4-methylpentan-1-ol, or a salt thereof,
- wherein the compound is (2R)-2-[(2-amino-5-{[(1S)-1-phenylethyl]thio}[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-4-methylpentan-1-ol, or a salt thereof, with a chiral purity of greater than 99.2%, and
- wherein the compound is prepared according to a process comprising the steps of:
- preparing a compound of formula I,
- via
- (ii) a compound of formula II,
- wherein R6 represents C1-6 alkyl optionally substituted by one or more F, or phenyl optionally substituted by one or more groups selected from halo, methyl, and —NO2;
- obtained by reacting a compound of formula III
- with a suitable sulfonating agent in the presence of a suitable base B1 and a suitable solvent S1, and subsequently
- (iii) reacting the compound of formula II, with a compound of formula IV,
- wherein M+ represents Lit, Nat, K+ or Cs+, and
- wherein the compound of formula III is provided as a single enantiomer.
8 more elements
A pharmaceutical formulation comprising the compound as claimed in claim 1, or a salt thereof.
Dependencies are inferred from the claim text.