Submission Details

Molecule(s):
CNC(=O)CN1C(=O)c2ccc(Cl)cc2C(C(=O)Nc2cncc3cc(S(C)(=O)=O)ccc23)C1C

EDG-MED-ee636701-1

CNC(=O)CN1C(=O)c2ccc(Cl)cc2C(C(=O)Nc2cncc3cc(S(C)(=O)=O)ccc23)C1C

CNC(=O)CN1C(=O)c2ccc(Cl)cc2C(C(=O)Nc2cncc3cc(F)ccc23)C1C

EDG-MED-ee636701-2

CNC(=O)CN1C(=O)c2ccc(Cl)cc2C(C(=O)Nc2cncc3cc(F)ccc23)C1C

CNC(=O)CN1C(=O)c2ccc(Cl)cc2C(C(=O)Nc2cncc3cc(Cl)ccc23)C1C

EDG-MED-ee636701-3

CNC(=O)CN1C(=O)c2ccc(Cl)cc2C(C(=O)Nc2cncc3cc(Cl)ccc23)C1C

CC1C(C(=O)Nc2cncc3cc(F)ccc23)c2cc(Cl)ccc2C(=O)N1CC(=O)NC1COC1

EDG-MED-ee636701-4

CC1C(C(=O)Nc2cncc3cc(F)ccc23)c2cc(Cl)ccc2C(=O)N1CC(=O)NC1COC1


Design Rationale:

methyl on P2 dihydroisoquinolone prevents racemisation. Mixture of cis and trans equilibrates to all cis, as amide prefers axial orientation and trans isomer is axial-axial.

Discussion: