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2,4-Dichloropyridine → N-(4-chloro-2-pyridinyl)-1,3-oxazol-2-amine

HRID 358
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HRID 358 반응식
Clc1ccnc(Cl)c1.Nc1ncco1>C1COCCO1.COc1ccc(OC)c(P(c2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2cc(C(F)(F)F)cc(C(F)(F)F)c2)c1-c1c(C(C)C)cc(C(C)C)cc1C(C)C.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C([O-])[O-].[Cs+].[Cs+].[Pd].[Pd]>Clc1ccnc(Nc2ncco2)c1
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참가 물질

7

반응물 2

HCID 335152,4-DichloropyridineHCID 5585212-Aminooxazole

생성물 1

HCID 130016260N-(4-chloro-2-pyridinyl)-1,3-oxazol-2-amine수율 0%

시약·촉매·용매 4

HCID 10796Cesium carbonate시약HCID 9811564Bis(dibenzylideneacetone)palladium촉매
HCID 44597232
Bis(3,5-bis(trifluoromethyl)phenyl)(3,6-dimethoxy-2',4',6'-tri(propan-2-yl)(1,1'-biphenyl)-2-yl)phosphane
촉매
HCID 312751,4-Dioxane용매

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온도
140 °C

실험 절차

Objective: Reactions using ligands not previously tested under these conditions 2,4-dichloropyridine (0.109 mL, 1.01 mmol), oxazol-2-amine (85 mg, 1.01 mmol), TRIS(DIBENZYLIDENEACETONE)DIPALLADIUM(0) (23.20 mg, 0.03 mmol), bis(3,5-bis(trifluoromethyl)phenyl)(2',4',6'-triisopropyl-3,6-dimethoxybiphenyl-2-yl)phosphine (81 mg, 0.10 mmol) and cesium carbonate (660 mg, 2.03 mmol) were added to an oven-dried microwave vail and the vial was purged with nitrogen. Degassed dioxane (4mL) was then added and the reaction mixture was heated to 140 °C for 1 h under microwave irradiation. Conclusion: None of the desired product was observed in the LCMS of the crude reaction mixture, not progressed.

출처 및 근거

ORD 기록
ord-de391e2f60334b77bfa7be520f63a36b
출처 데이터셋
750 AstraZeneca ELN dataset
원본 링크
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