2-AMino-7-Boc-7-azaspiro[...

tert- uty] 2-amino-7-azaspiro[3.5]nonane-7-carboxylate (480.7 mg, 2.0 rnmol, 1 .0 eq.) was dissolved m H-BUOH (10.0 raL, 0.2 M), and DIPEA (1 , 045 raL, 6.0 rnmol, 3, 0 eq.) was added followed by 3, 6-dichloropyridazine (893.9 mg, 6.0 rnmol, 3.0 eq.). The reaction mixture was stirred at 100 °C overnight, after which time the reaction was cooled to r.t. , and diluted with DCM and sat. soln. NaHCCb. The aqueous layer was extracted with iPA/CHCb (1 :3, 3x). The combined extracts were dried over Na2S04, filtered and concentrated. The crude residue was purified by flash column chromatography on silica gel (0-50percent EtOAc/hexanes then 50-80percent EtOAc/DCM) to provide the title compound as a white crystalline solid (300 mg, 43percent). 1H- NMR (400 MHz, CDCb) delta 7.18 (d, J = 9.2 Hz, 1H), 6.59 i d. J = 9.7 Hz, 1 1 1 ). 5.08 (br, I I I ). 4.28 (d. ./ 6.2 Hz, lH), 3.40 (dd, J = 5.5, 5.5 Hz, 2H), 3.32 (do. ./ 5.5, 5.5 Hz, 2H), 2.47 (ddd, 10.2, 7.9, 2.5 Hz, 21 1 ). 1.70 (ddd, 10.2, 7.9, 2, 6 Hz, 2H), 1.63 (dd, J = 5.6, 5.6 Hz, 2H), 1.56 (del, J 5.6, 5.6 Hz, 2H), 1.47 (s, 9H); ES-MS | M i l l | i · Eta Gamma -- iBuiv = 186.3.Take compound 6-7 (350 mg, 1.46 mmol), For sulfonamide benzoic acid (352 mg, 1.75 mmol, 1.2 eq.), HOBt (591 mg, 4.38 mmol, 3 equivalents) and EDCI (840 mg, 4.38 mmol, 3 equivalents) in a 25 mL single-mouth bottle, DMF andTEA (1 mL, 7.3 mmol, 5 eq.). Stir at room temperature.TLC tracking monitoring. Rotate DMF, add EA and water extraction, Wash with saturated brine, dry, spin dry, and pass through a column (DCM:acetone = 2.5:1).White solid product 400mg

Molecular Weight:240.34
XLogP3:1.3
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:2
Exact Mass:240.183778013
Monoisotopic Mass:240.183778013
Topological Polar Surface Area:55.6
Heavy Atom Count:17
Complexity:293
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes