(2R)-2-amino-2,3-dimethylbutan-1-ol

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: The title compound was synthesized in analogy to Example 1, using 5-cyclopropyl-6-cyclopropylmethoxy-pyridine-2-carboxylic acid (Example 42 a) and (R)-2-amino-2,3-dimethyl-butan-1-ol [CAN 155158-75-1] as starting materials, MS (EI): m/e=333.2 [M+H]+.

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: The title compound was synthesized in analogy to Example 1, using 5-cyclopropyl-6-cyclopropylmethoxy-pyridine-2-carboxylic acid (Example 42 a) and (R)-2-amino-2,3-dimethyl-butan-1-ol [CAN 155158-75-1] as starting materials, MS (EI): m/e=333.2 [M+H]+.

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: The title compound was synthesized in analogy to Example 1, using 5-cyclopropyl-6-cyclopropylmethoxy-pyridine-2-carboxylic acid (Example 42 a) and (R)-2-amino-2,3-dimethyl-butan-1-ol [CAN 155158-75-1] as starting materials, MS (EI): m/e=333.2 [M+H]+.

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: The title compound was synthesized in analogy to Example 1, using 5-chloro-4-(4-fluorobenzyl)-pyridine-2-carboxylic acid and (2R)-2-amino-2,3-dimethyl-1-butanol (CAN 155158-75-1) as starting materials and isolated (29 mg, 25%) as colorless oil; LC-MS (UV peak area, m/z) 100%, 365.1428 (MH+). isolated (29 mg, 25%) as colorless oil

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: The title compound was synthesized in analogy to Example 1, using 5-chloro-4-cyclopropylmethoxy-pyridine-2-carboxylic acid and (2R)-2-amino-2,3-dimethyl-1-butanol (CAN 155158-75-1) as starting materials and isolated (19 mg, 19%) as colorless oil; LC-MS (UV peak area, m/z) 98.6%, 327.1464 (MH+). isolated (19 mg, 19%) as colorless oil

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a solution of 5-chloro-4-cyclobutylmethoxy-pyridine-2-carboxylic acid (60 mg, 249 μmol) in acetonitrile (2 mL) was added HATU (123 mg, 324 μmol), (2R)-2-amino-2,3-dimethyl-1-butanol (CAN 155158-75-1, 32.1 mg, 274 μmol) and DIEA (217 μL, 1.25 mmol). The brownish reaction mixture was stirred for 18 h at room temperature. The crude reaction mixture was concentrated in vacuo and the residue was purified by flash chromatography (silica, heptane/ethyl acetate gradient) and finally chiral chromatography (ChiralPak AD, heptane/ethanol 9:1) to deliver the desired compound (27.3 mg, 43%) as colorless oil. MS (ESI, m/z): 341.1 (MH+). The brownish reaction mixture The crude reaction mixture was concentrated in vacuo the residue was purified by flash chromatography (silica, heptane/ethyl acetate gradient) and finally chiral chromatography (ChiralPak AD, heptane/ethanol 9:1)

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: The title compound was synthesized in analogy to Example 15, using 5-cyclopropyl-6-cyclopropylmethoxy-pyrazine-2-carboxylic acid (Example 10 g; 100 mg, 0.42 mmol) and (2R)-2-amino-2,3-dimethyl-1-butanol (CAN 155158-75-1, 107.06 mg, 0.64 mmol) as starting materials, and isolated (20 mg, 14.04%) as off white sticky solid, LC-MS (UV peak area, ESI) 100%, 334.4 (M+H). isolated (20 mg, 14.04%) as off white sticky solid, LC-MS (UV peak area, ESI) 100%, 334.4 (M+H)

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: The title compound was synthesized in analogy to Example 1, using 5-cyclopropyl-6-cyclopropylmethoxy-pyridine-2-carboxylic acid (Example 42 a) and (R)-2-amino-2,3-dimethyl-butan-1-ol [CAN 155158-75-1] as starting materials, MS (EI): m/e=333.2 [M+H]+.

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: The title compound was synthesized in analogy to Example 1, using 5-cyclopropyl-6-cyclopropylmethoxy-pyridine-2-carboxylic acid (Example 42 a) and (R)-2-amino-2,3-dimethyl-butan-1-ol [CAN 155158-75-1] as starting materials, MS (EI): m/e=333.2 [M+H]+.