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US 2022/0064205 A1Published application
Process for the preparation of a cyclic dinucleotide
AssigneeBristol-Myers Squibb Company
InventorsMichael Anthony Schmidt, Bin Zheng Kendall Park, Benjamin M. Cohen, Amanda J. Rogers, Changxia Yuan Warren, Jason J. Zhu, Chao Hang, Daniel S. Treitler, Adam Josep Freitag, Geoffrey Eugene Purdum, Miao Yu, Melda Sezen Edmonds, Siwei Guo
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Abstract
The invention generally relates to an improved processes for the preparation of a cyclic dinucleotide which is useful as a STING agonist of the following formula (I), involving the use of compounds A and B.
Claims18
A process for the preparation of Compound I of the formula
- comprising the steps of
- a) reacting Compound 1 with TBSCl and Et3N
- to afford Compound 2;
- b) reacting Compound 2 with Compound A to afford Compound 3
- c) reacting Compound 3 and Compound 9
- to afford Compound 4;
- d) reacting Compound 4 in a solvent, and then adding a base, followed by the addition of Compound B, to afford Compound 5 of the formula
- e) selectively deprotecting Compound 5 to afford Compound 6 of the formula
- f) which is cyclized in a suitable solvent under basic conditions to afford Compound 7 of the formula
- g) which is subsequently mixed in a suitable base, stirred and concentrated to afford Compound 8 of the formula
- which is subsequently deprotected to afford Compound I.
8 more elements
A compound as shown in the table below;
- Compound No.
- Structure
- 2
- 3
- 4
- 5
- 6
- 7
- 8
- and diastereomers thereof.
7 more elements
Dependencies are inferred from the claim text.