## 3 Materials and Methods
### Chemical Syntheses
#### 3.2.5 Preparation of Phenyl(4-benzyloxy)-7-morpholinobenzo[_d_]thiazol-2-yl)carbamate (6)
The resulting mixture was stirred for 10 min and then extracted with ethyl acetate (2 \(\times\) 75 mL). The combined extracts were washed with saturated aqueous sodium bicarbonate (50 mL) and brine (100 mL) and dried over anhydrous Na\({}_{2}\)SO\({}_{4}\). Subsequent evaporation of the solvent furnished a solid, which was recrystallized from 80% aqueous MeOH to afford the analytically pure title compound (187 mg, 74%) as a light grey solid, mp 246 \({}^{\circ}\)C.  
\({}^{1}\)H-NMR (400 MHz, DMSO-\(d_{6}\)) 8.16 (s, 3H, CH\({}_{3}\)), 1.37 (s, 9H, C(CH\({}_{3}\))\({}_{3}\)), 1.40-1.58 (m, 4H, Pip-C\({}^{3}\)\(H_{2}\) + Pip-C\({}^{5}\)\(H_{2}\)), 3.08 (t, 4H, \(J\) = 45 Hz, CH\({}_{2}\)NCH\({}_{2}\)), 3.21-3.36 (m, 2H, 0.5 Pip-C\({}^{2}\)\(H_{2}\) + 0.5 Pip\({}^{6}\)\(H_{2}\)), 3.79 (t, 4H, \(J\) = 45 Hz, CH\({}_{2}\)OCH\({}_{2}\)), 3.76-3.91 (m, 2H, 0.5 Pip-C\({}^{2}\)\(H_{2}\) + 0.5 Pip-C\({}^{6}\)\(H_{2}\)), 4.40 (s\({}_{\rm br}\), 1H, OH), 6.83 (d, 2H, \(H^{6}\)), 6.99 (d, 2H, \(H^{5}\)), 10.93 (s, 1H, NH), \({}^{13}\)C-NMR (100 MHz, DMSO-\(d_{6}\)) 827.4 (C(CH\({}_{3}\))\({}_{3}\)), 30.1 (CH\({}_{3}\)), 38.5 (Pip-C\({}^{3.5}\)), 39.0 (C(CH\({}_{3}\))\({}_{3}\)), 40.9 (Pip-C\({}^{2.6}\)), 51.5 (CNC), 66.3 (Pip-C\({}^{4}\)), 66.8 (COC), 111.8 (C\({}^{6}\)), 119.6 (C\({}^{5}\)), 130.5 (C\({}^{7a}\)), 141.9 (C\({}^{3a}\)), 144.3 (C\({}^{7}\)), 146.3 (C\({}^{4}\)), 150.9 (C=O), 160.3 (C\({}^{2}\)), 177.3 (Piv C=O). Anal. calcd for C\({}_{23}\)H\({}_{32}\)N\({}_{4}\)O\({}_{5}\)S: C, 57.96; H, 6.77; N, 11.76; found: C, 57.93; H, 6.79; N, 11.77. HRMS \(m/z\): [M + H]\({}^{+}\) calcd: 477.2166; found: 477.2158. 3.2.12. Preparation of _tert_-Butyl (4-(benzyloxy)-7-morpholinobenzo[\(d\)]thiazol-2-yl)(4-hydroxy-4-methylpiperidine-1-carbonyl)carbamate (**11**)  
Triethylamine (210 uL, 3 equiv) and di-_tert_-butyl dicarbonate (218 mg, 1 mmol, 2 equiv) were added to a well-stirred suspension of 7 (241 mg, 0.5 mmol, 1 equiv) in anhydrous THF (6 mL). 4-(Dimethylamine)pyridine (61 mg, 0.5 mmol, 0.5 equiv) was added and the reaction mixture was stirred for 10 min (TLC: ethyl acetate/hexane, 80/20, R\({}_{\rm fs.m. }\) 0.35, R\({}_{\rm fp}\) 0.76), during which the color of the solution changed to orange and then yellow. The reaction was quenched by addition of saturated aqueous sodium bicarbonate (10 mL), and the resulting mixture was extracted with dichloromethane (2 \(\times\) 40 mL). The combined extracts were washed with 1% aqueous HCl (50 mL), water (50 mL) and brine (50 mL) and dried over anhydrous Na\({}_{2}\)SO\({}_{4}\). Subsequent evaporation of the solvent under reduced pressure afforded the title compound (260 mg, 89%) as off-white crystals, mp 91 \({}^{\circ}\)C.  
\({}^{1}\)H-NMR (400 MHz, DMSO-\(d_{6}\)) \(\delta\) 1.06 (s\({}_{br}\), 3H, CH\({}_{3}\)), 1.43-1.63 (m, 4H, Pip-C\({}^{3}H_{2}\) + Pip-C\({}^{5}H_{2}\)), 1.52 (s, 9H, Boc-CH\({}_{3}\)), 3.03 (t, 4H, \(J\) = 4.5 Hz, CH\({}_{2}\)NCH\({}_{2}\)), 3.25-3.44 (m, 3H, 0.5 Pip-C\({}^{2}H_{2}\) + 0.5 Pip-C\({}^{6}H_{2}\) + 0.5 Pip-C\({}^{2/6}H_{2}\)), 3.78 (t, 4H, \(J\) = 4.5 Hz, CH\({}_{2}\)OCH\({}_{2}\)), 3.84 + 4.04 (s\({}_{br}\), 1H, 0.5 Pip- C\({}^{2/6}H_{2}\)), 4.51 (s\({}_{br}\), 1H, OH), 5.26 (s, 2H, Bn-CH\({}_{2}\)), 6.94 (d, 1H, \(J\) = 8.5 Hz, \(H^{6}\)), 7.03 (d, 1H, \(J\) = 8.5 Hz, \(H^{5}\)), 7.28-7.50 (m, 5H, C\({}_{6}H_{5}\)). \({}^{13}\)C-NMR (100 MHz, DMSO-\(d_{6}\)) \(\delta\) 28.0 (Boc CH\({}_{3}\)), 30.2 (CH\({}_{3}\)), 51.9 (CNC), 66.0 (Pip-C\({}^{4}\)), 67.0 (COC), 71.3 (Bn-CH\({}_{2}\)), 85.1 (Boc C), 114.1 (C\({}^{5/6}\)), 122.0 (Bn-C\({}^{1}\)), 125.6 (\(C^{2}\)), 127.8, 128.2, 128.8, (Bn-C\({}^{2,3,4}\)), 137.8 (C\({}^{1a}\)), 140.8 (C\({}^{7}\)), 147.6 (C\({}^{1}\)), 149.0 (\(C^{2}\)), 150.3 (Boc C=O), 156.3 (Pip C=O)(signals for the piperidine methylene carbons are missing). Anal. calcd for C\({}_{30}\)H\({}_{38}\)N\({}_{4}\)O\({}_{6}\)S: C, 61.84; H, 6.57; N, 9.61; found: C, 61.79; H, 6.61; N, 9.57. HRMS \(m/z\): [M + H]\({}^{+}\) calcd: 583.2585; found: 583.2583.