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US 2021/0198296 A1Published application
Processes for preparing oligomers
AssigneeSarepta Therapeutics, Inc.
InventorsBaozhong CAI, Mitchell MARTINI, Ross SHIMABUKU, Katie THOMAS, Diane Elizabeth FRANK, Richard K. BESTWICK
Life of this patent
Estimating the term…
Abstract
Provided herein are processes for preparing an oligomer (e.g., a morpholino oligomer). The synthetic processes described herein may be advantageous to sealing up oligomer synthesis while maintaining overall yield and parity of a synthesized oligomer.
Claims10
1-27. (canceled)
A compound of Formula (B1):
- or a pharmaceutically acceptable salt thereof
- wherein
- R11 is selected from the group consisting of halo, CN, and NO2;
- R12 is C1-6-alkyl;
- R13 is H or C1-6-alkyl;
- and
- R14 is a first linker bound to a support-medium,
- R3 is selected from the group consisting of trityl, monomethoxytrityl, dimethoxytrityl and trimethoxytrityl.
5 more elements
A compound of Formula (II-B):
- or a pharmaceutically acceptable salt thereof
- wherein
- R11 is selected from the group consisting of halo, CN, and NO2;
- R12 is C1-6-alkyl;
- R13 is H or C1-6-alkyl;
- and
- R14 is a first linker bound to a support-medium.
4 more elements
A compound of Formula (B3):
- or a pharmaceutically acceptable salt thereof
- wherein
- w is selected from O or C;
- t is 1, 2, 3, 4, or 5;
- R11 is selected from the group consisting of halo, CN, and NO2;
- R12 is C1-6-alkyl;
- R13 is H or C1-6-alkyl;
- R14 is a first linker bound to a support-medium;
- R8 is selected from:
- wherein R4 is selected from the group consisting of:
- and
- R3 is selected from the group consisting of trityl, monomethoxytrityl, dimethoxytrityl and trimethoxytrityl.
9 more elements
A compound selected from:
- wherein:
- n is an integer from 10 to 40;
- R1 is a support-medium;
- R3 is selected from the group consisting of trityl, monomethoxytrityl, dimethoxytrityl and trimethoxytrityl;
- and
- R4 is, independently at each occurrence, selected from the group consisting of:
3 more elements
A compound selected from:
- wherein:
- R11 is selected from the group consisting of halo, CN, and NO2;
- R12 is C1-6-alkyl;
- R13 is H or C1-6-alkyl;
- R14 is a first linker bound to a support-medium;
- R1 is selected from —O(C1-C6alkyl), halo, —O(C1-C6alkyl)-O(C1-C6alkyl), and —O(C1-C6alkyl)-C(O)—NH—C1-C6alkyl
- R2 is H or R1 and R2 join to form a cycloalkyl or heterocyclic ring having from 4 to 7 ring atoms optionally containing an oxygen;
- R5, R6, and R7 are each hydrogen, or R5 and R7 join to form a cycloalkyl ring having from 4 to 7 ring atoms and R6 and R7 join to for a cycloalkyl ring having from 3 to 4 ring atoms,
- R9 is —OCH2CH2CN or —CH2C(═O)OC(CH3)2CH2CN;
- R4 is, independently at each occurrence, selected from the group consisting of:
- R8 is, independently at each occurrence, selected from the group consisting of H, trityl, monomethoxytrityl, dimethoxytrityl and trimethoxytrityl;
- n is 10 to 40;
- and
- X is O or S.
11 more elements
36-37. (canceled)
Dependencies are inferred from the claim text.