1: 99 percent / NH3, Na, t-BuOH / tetrahydrofuran / 1.) -78 deg C, 6 min, 2.) -78 to -33 deg C, 2 min 2: 100 percent / 4-DMAP, pyridine / 36 h 3: 98 percent / NaBH4 / methanol / 2.5 h 4: 94 percent / DIEA / CH2Cl2 / 6 h 5: 100 percent / TBAF / tetrahydrofuran / 24 h 6: 69 percent / 4-DMAP / acetonitrile / 11.5 h 7: 0.25 h / 24 - 200 °C / 12 Torr 8: DIEA / methanol / 2 h 9: 93 percent / 2 N aq. HCl / methanol / 23 h / Heating 10: 100 percent / DIEA / methanol / 4 h View Scheme

1: 99 percent / KHMDS / tetrahydrofuran / 1.) -50 to -35 deg C, 15 min, 2.) -35 deg C, 40 min 2: 99 percent / NH3, Na, t-BuOH / tetrahydrofuran / 1.) -78 deg C, 6 min, 2.) -78 to -33 deg C, 2 min 3: 100 percent / 4-DMAP, pyridine / 36 h 4: 98 percent / NaBH4 / methanol / 2.5 h 5: 94 percent / DIEA / CH2Cl2 / 6 h 6: 100 percent / TBAF / tetrahydrofuran / 24 h 7: 69 percent / 4-DMAP / acetonitrile / 11.5 h 8: 0.25 h / 24 - 200 °C / 12 Torr 9: DIEA / methanol / 2 h 10: 93 percent / 2 N aq. HCl / methanol / 23 h / Heating 11: 100 percent / DIEA / methanol / 4 h View Scheme

1: 93 percent / CBr4, PPh3 / CH2Cl2 / 1.) 0 deg C to r.t., 1 h, 2.) r.t., 13 h 2: 99 percent / KHMDS / tetrahydrofuran / 1.) -50 to -35 deg C, 15 min, 2.) -35 deg C, 40 min 3: 99 percent / NH3, Na, t-BuOH / tetrahydrofuran / 1.) -78 deg C, 6 min, 2.) -78 to -33 deg C, 2 min 4: 100 percent / 4-DMAP, pyridine / 36 h 5: 98 percent / NaBH4 / methanol / 2.5 h 6: 94 percent / DIEA / CH2Cl2 / 6 h 7: 100 percent / TBAF / tetrahydrofuran / 24 h 8: 69 percent / 4-DMAP / acetonitrile / 11.5 h 9: 0.25 h / 24 - 200 °C / 12 Torr 10: DIEA / methanol / 2 h 11: 93 percent / 2 N aq. HCl / methanol / 23 h / Heating 12: 100 percent / DIEA / methanol / 4 h View Scheme

1: 100 percent / H2 / 10percent Pd/C / ethanol / 23 h 2: 93 percent / CBr4, PPh3 / CH2Cl2 / 1.) 0 deg C to r.t., 1 h, 2.) r.t., 13 h 3: 99 percent / KHMDS / tetrahydrofuran / 1.) -50 to -35 deg C, 15 min, 2.) -35 deg C, 40 min 4: 99 percent / NH3, Na, t-BuOH / tetrahydrofuran / 1.) -78 deg C, 6 min, 2.) -78 to -33 deg C, 2 min 5: 100 percent / 4-DMAP, pyridine / 36 h 6: 98 percent / NaBH4 / methanol / 2.5 h 7: 94 percent / DIEA / CH2Cl2 / 6 h 8: 100 percent / TBAF / tetrahydrofuran / 24 h 9: 69 percent / 4-DMAP / acetonitrile / 11.5 h 10: 0.25 h / 24 - 200 °C / 12 Torr 11: DIEA / methanol / 2 h 12: 93 percent / 2 N aq. HCl / methanol / 23 h / Heating 13: 100 percent / DIEA / methanol / 4 h View Scheme

1: 92 percent / imidazole / dimethylformamide / 15 h 2: 99 percent / NaH, TBAI / tetrahydrofuran / 1.) 15 min, 2.) 42 h 3: 100 percent / H2 / 10percent Pd/C / ethanol / 23 h 4: 93 percent / CBr4, PPh3 / CH2Cl2 / 1.) 0 deg C to r.t., 1 h, 2.) r.t., 13 h 5: 99 percent / KHMDS / tetrahydrofuran / 1.) -50 to -35 deg C, 15 min, 2.) -35 deg C, 40 min 6: 99 percent / NH3, Na, t-BuOH / tetrahydrofuran / 1.) -78 deg C, 6 min, 2.) -78 to -33 deg C, 2 min 7: 100 percent / 4-DMAP, pyridine / 36 h 8: 98 percent / NaBH4 / methanol / 2.5 h 9: 94 percent / DIEA / CH2Cl2 / 6 h 10: 100 percent / TBAF / tetrahydrofuran / 24 h 11: 69 percent / 4-DMAP / acetonitrile / 11.5 h 12: 0.25 h / 24 - 200 °C / 12 Torr 13: DIEA / methanol / 2 h 14: 93 percent / 2 N aq. HCl / methanol / 23 h / Heating 15: 100 percent / DIEA / methanol / 4 h View Scheme

1: 99 percent / NaH, TBAI / tetrahydrofuran / 1.) 15 min, 2.) 42 h 2: 100 percent / H2 / 10percent Pd/C / ethanol / 23 h 3: 93 percent / CBr4, PPh3 / CH2Cl2 / 1.) 0 deg C to r.t., 1 h, 2.) r.t., 13 h 4: 99 percent / KHMDS / tetrahydrofuran / 1.) -50 to -35 deg C, 15 min, 2.) -35 deg C, 40 min 5: 99 percent / NH3, Na, t-BuOH / tetrahydrofuran / 1.) -78 deg C, 6 min, 2.) -78 to -33 deg C, 2 min 6: 100 percent / 4-DMAP, pyridine / 36 h 7: 98 percent / NaBH4 / methanol / 2.5 h 8: 94 percent / DIEA / CH2Cl2 / 6 h 9: 100 percent / TBAF / tetrahydrofuran / 24 h 10: 69 percent / 4-DMAP / acetonitrile / 11.5 h 11: 0.25 h / 24 - 200 °C / 12 Torr 12: DIEA / methanol / 2 h 13: 93 percent / 2 N aq. HCl / methanol / 23 h / Heating 14: 100 percent / DIEA / methanol / 4 h View Scheme

1: 62 percent / TMSN3, (+)-(1S,2S)-bis<2'-(diphenylphosphino)benzamido>-1,2-diphenylethane / Pd2(dba)3*CHCl3 / tetrahydrofuran / 1.5 h / -78 °C 2: PPh3 / tetrahydrofuran; H2O / 14 h / Ambient temperature 3: K2CO3 / tetrahydrofuran; H2O / 24 h / Ambient temperature 4: 96 percent / PPh3 / Pd2(dba)3*CHCl3 / tetrahydrofuran / 2 h / Ambient temperature 5: 47 percent / DBU, TBA oxone, Cs2CO3 / CH2Cl2 / 1.) r.t., 30 min, 2.) sonication, 4 h; r.t., 40 h 6: 73 percent / LiBH4 / diethyl ether / 2 h / Ambient temperature View Scheme

1: 97 percent / PPh3, imidazole, I2 / toluene / 1.) 60 deg C, 10 min, 2.) reflux, 3.75 h 2: 98 percent / DBU / xylene / 16.5 h / Heating 3: CAN / acetonitrile; H2O / 0.28 h / 0 °C 4: DMAP, pyridine / 22 h 5: 93 percent / NaBH4 / methanol / 2.5 h View Scheme

1: 97 percent / TBAF / tetrahydrofuran / 0.33 h 2: 97 percent / PPh3, imidazole, I2 / toluene / 1.) 60 deg C, 10 min, 2.) reflux, 3.75 h 3: 98 percent / DBU / xylene / 16.5 h / Heating 4: CAN / acetonitrile; H2O / 0.28 h / 0 °C 5: DMAP, pyridine / 22 h 6: 93 percent / NaBH4 / methanol / 2.5 h View Scheme

1: 89 percent / CBr4, PPh3 / CH2Cl2 / 1.) 0 deg C to r.t., 1 h, 2.) r.t., 22 h 2: 90 percent / KHMDS / tetrahydrofuran / 1.) -50 to -35 deg C, 15 min, 2.) -35 deg C, 40 min 3: 97 percent / TBAF / tetrahydrofuran / 0.33 h 4: 97 percent / PPh3, imidazole, I2 / toluene / 1.) 60 deg C, 10 min, 2.) reflux, 3.75 h 5: 98 percent / DBU / xylene / 16.5 h / Heating 6: CAN / acetonitrile; H2O / 0.28 h / 0 °C 7: DMAP, pyridine / 22 h 8: 93 percent / NaBH4 / methanol / 2.5 h View Scheme