N-methyl-2-morpholin-4-ylacetamide → N-methyl-2-morpholin-4-yl-N-[6-(2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidin-9-yl)dibenzothiophen-2-yl]acetamide

HRID 201

반응식

HRID 201 반응식
CNC(=O)CN1CCOCC1.O=c1cc(N2CCOCC2)nc2c(-c3cccc4c3sc3ccc(OS(=O)(=O)C(F)(F)F)cc34)cccn12>CC(=O)O.CC(=O)O.Cc1ccccc1.O=P([O-])([O-])[O-].[K+].[K+].[K+].[Pd].c1ccc(P(c2ccccc2)c2ccc3ccccc3c2-c2c(P(c3ccccc3)c3ccccc3)ccc3ccccc23)cc1>CN(C(=O)CN1CCOCC1)c1ccc2sc3c(-c4cccn5c(=O)cc(N6CCOCC6)nc45)cccc3c2c1

참가 물질

7

반응물 2

HCID 22031405N-methyl-2-morpholin-4-ylacetamideHCID 87563685[6-(2-Morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidin-9-yl)dibenzothiophen-2-yl] trifluoromethanesulfonate

생성물 1

HCID 68758915N-methyl-2-morpholin-4-yl-N-[6-(2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidin-9-yl)dibenzothiophen-2-yl]acetamide수율 0%

시약·촉매·용매 4

HCID 62657Potassium Phosphate, Tribasic시약HCID 634876Binap, (A+-)-촉매HCID 4144353Palladium (II) acetate촉매HCID 1140Toluene용매

반응 조건

온도
110 °C

실험 절차

In a microwave vial, under nitrogen, at room temperature, a solution of 6-(2-morpholino-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl)dibenzo[b,d]thiophen-2-yl trifluoromethanesulfonate (63 mg, 0.11 mmol) in dry toluene (1 mL) was added to a stirred mixture of N-methyl-2-morpholinoacetamide (35.5 mg, 0.22 mmol), Tripotassium phosphate (47.6 mg, 0.22 mmol), rac BINAP (6.99 mg, 0.01 mmol) and Palladium(II) acetate (2.52 mg, 0.01 mmol) in . The resulting mixture was heated in a Biotage Optimiser Microwave reactor under nitrogen at 100 °C for 3 hours. UPLC of the reaction showed no indication of the desired compound - not isolated - reaction abandonned.

출처 및 근거

ORD 기록
ord-cddf8b0bbaa34d7fad426cd90b95c72f
출처 데이터셋
750 AstraZeneca ELN dataset
원본 링크
출처 보기

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