Technology Process of (2R)-5-(2-{[(8R)-8-(3,5-difluorophenyl)-8-methyl-10-oxo-6,9-diazaspiro[4,5]dec-9-yl]methyl}cyclopropyl)-1,3-dihydrospiro[indene-2,3'-pyrrolo[2,3-b]pyridin]-2'(1'H)-one trifluoroacetate salt
There total 12 articles about (2R)-5-(2-{[(8R)-8-(3,5-difluorophenyl)-8-methyl-10-oxo-6,9-diazaspiro[4,5]dec-9-yl]methyl}cyclopropyl)-1,3-dihydrospiro[indene-2,3'-pyrrolo[2,3-b]pyridin]-2'(1'H)-one trifluoroacetate salt which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
C40H48F2N4O3Si;
With
ethylenediamine; sodium hydroxide;
In
methanol; water;
for 0.5h;
pH=10;
trifluoroacetic acid;
In
water; acetonitrile;
- Guidance literature:
-
Multi-step reaction with 8 steps
1.1: pyridinium hydrobromide perbromide / 1,4-dioxane / 1 h / 20 °C
2.1: water
3.1: ammonium chloride; zinc / tetrahydrofuran; water / 3 h
4.1: caesium carbonate / methanol / 18 h
5.1: sodium acetate / tris(o-methoxyphenyl)phosphine; palladium diacetate / N,N-dimethyl-formamide / 1 h / 130 °C / Microwave irradiation
6.1: potassium hydroxide / diethyl ether; water / 0.25 h / -78 °C
6.2: 18 h / 20 °C
7.1: trifluoroacetic acid / 0.5 h / 20 °C
8.1: ethylenediamine; sodium hydroxide / methanol; water / 0.5 h / pH 10
With
water; sodium acetate; pyridinium hydrobromide perbromide; ammonium chloride; caesium carbonate; ethylenediamine; trifluoroacetic acid; potassium hydroxide; sodium hydroxide; zinc;
tris(o-methoxyphenyl)phosphine; palladium diacetate;
In
tetrahydrofuran; 1,4-dioxane; methanol; diethyl ether; water; N,N-dimethyl-formamide;
- Guidance literature:
-
Multi-step reaction with 9 steps
1.1: sodium hydride / N,N-dimethyl-formamide; mineral oil / 1.42 h / 0 °C
1.2: 1.25 h / 10 °C
2.1: pyridinium hydrobromide perbromide / 1,4-dioxane / 1 h / 20 °C
3.1: water
4.1: ammonium chloride; zinc / tetrahydrofuran; water / 3 h
5.1: caesium carbonate / methanol / 18 h
6.1: sodium acetate / tris(o-methoxyphenyl)phosphine; palladium diacetate / N,N-dimethyl-formamide / 1 h / 130 °C / Microwave irradiation
7.1: potassium hydroxide / diethyl ether; water / 0.25 h / -78 °C
7.2: 18 h / 20 °C
8.1: trifluoroacetic acid / 0.5 h / 20 °C
9.1: ethylenediamine; sodium hydroxide / methanol; water / 0.5 h / pH 10
With
water; sodium acetate; pyridinium hydrobromide perbromide; sodium hydride; ammonium chloride; caesium carbonate; ethylenediamine; trifluoroacetic acid; potassium hydroxide; sodium hydroxide; zinc;
tris(o-methoxyphenyl)phosphine; palladium diacetate;
In
tetrahydrofuran; 1,4-dioxane; methanol; diethyl ether; water; N,N-dimethyl-formamide; mineral oil;