RO8994

Base Information

• Chemical Name: RO8994
• CAS No.: 1309684-94-3
• Molecular Formula: C₃₁H₃₁Cl₂FN₄O₄
• Molecular Weight: 613.516

Synonyms:RO8994;(2'S,3R,4'S,5'R)-N-[4-(Aminocarbonyl)-2-methoxyphenyl]-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-1,2-dihydro-2-oxo-spiro[3H-indole-3,3'-pyrrolidine]-5'-carboxamide

Chemical Property of RO8994

Chemical Property:

• Boiling Point: 753.5±60.0 °C(Predicted)
• PKA: 12.00±0.70(Predicted)
• Density: 1.41±0.1 g/cm3(Predicted)

Purity/Quality:

99%, ^*data from raw suppliers

RO8994 ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

SDS file from LookChem

Useful:

• Description: RO8994 is an inhibitor of the protein-protein interaction between MDM2 and the tumor suppressor p53 in a homogeneous time-resolved fluorescence (HTRF) binding assay (IC50 = 5 nM). It inhibits the proliferation of SJSA-1, RKO, and HCT116 cells with an average IC50 value of 20 nM and increases apoptosis in SJSA-1 cells in a concentration-dependent manner. RO8994 reduces tumor growth and induces tumor regression in an SJSA-1 osteosarcoma mouse xenograft model when administered at doses of 1.56 and 6.25 mg/kg, respectively.
• Uses: RO 8994 is a potent and selective spiroindolinone MDM2 inhibitor, and potential useful for cancer therapy.

Technology Process of RO8994

There total 21 articles about RO8994 which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield:

2-fluoro-3-chlorobenzaldehyde (85070-48-0) → (2'S,3'R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-2-oxo-1,2-dihydrospiro[indole-3,3'-pyrrolidine]-5'-carboxylic acid (4-carbamoyl-2-methoxyphenyl)amide (1309684-94-3)

Guidance literature:

Multi-step reaction with 6 steps

1.1: piperidine / methanol / 20 °C / Reflux

2.1: silver(I) acetate; (6,6’-dimethoxy-[1,1 ‘-biphenyl]-2,2’-diyl)bis(bis(3 ,5-dimethyl-phenyl)phosphine); triethylamine / 2-methyltetrahydrofuran / 28 h / 40 °C

2.2: Reflux

3.1: sodium hydroxide / tetrahydrofuran; water / 4 h / 65 °C

4.1: ethyl acetate / 4 h / 60 °C

5.1: tetrahydrofuran / 1.5 h / 20 °C

6.1: ammonium hydroxide / 0.5 h / 20 °C

With piperidine; ammonium hydroxide; (6,6’-dimethoxy-[1,1 ‘-biphenyl]-2,2’-diyl)bis(bis(3 ,5-dimethyl-phenyl)phosphine); silver(I) acetate; triethylamine; sodium hydroxide; In tetrahydrofuran; 2-methyltetrahydrofuran; methanol; water; ethyl acetate;

DOI:10.1021/op3003213

Reference yield:

6-chloro-3-[1-(3-chloro-2-fluorophenyl)-meth-(E)-ylidene]-1,3-dihydroindol-2-one (908027-64-5) → (2'S,3'R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-2-oxo-1,2-dihydrospiro[indole-3,3'-pyrrolidine]-5'-carboxylic acid (4-carbamoyl-2-methoxyphenyl)amide (1309684-94-3)

Guidance literature:

Multi-step reaction with 5 steps

1.1: silver(I) acetate; (6,6’-dimethoxy-[1,1 ‘-biphenyl]-2,2’-diyl)bis(bis(3 ,5-dimethyl-phenyl)phosphine); triethylamine / 2-methyltetrahydrofuran / 28 h / 40 °C

1.2: Reflux

2.1: sodium hydroxide / tetrahydrofuran; water / 4 h / 65 °C

3.1: ethyl acetate / 4 h / 60 °C

4.1: tetrahydrofuran / 1.5 h / 20 °C

5.1: ammonium hydroxide / 0.5 h / 20 °C

With ammonium hydroxide; (6,6’-dimethoxy-[1,1 ‘-biphenyl]-2,2’-diyl)bis(bis(3 ,5-dimethyl-phenyl)phosphine); silver(I) acetate; triethylamine; sodium hydroxide; In tetrahydrofuran; 2-methyltetrahydrofuran; water; ethyl acetate;

DOI:10.1021/op3003213

Reference yield:

6-chloro-2-oxindole (56341-37-8) → (2'S,3'R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-2-oxo-1,2-dihydrospiro[indole-3,3'-pyrrolidine]-5'-carboxylic acid (4-carbamoyl-2-methoxyphenyl)amide (1309684-94-3)

Guidance literature:

Multi-step reaction with 6 steps

1.1: piperidine / methanol / 20 °C / Reflux

2.1: silver(I) acetate; (6,6’-dimethoxy-[1,1 ‘-biphenyl]-2,2’-diyl)bis(bis(3 ,5-dimethyl-phenyl)phosphine); triethylamine / 2-methyltetrahydrofuran / 28 h / 40 °C

2.2: Reflux

3.1: sodium hydroxide / tetrahydrofuran; water / 4 h / 65 °C

4.1: ethyl acetate / 4 h / 60 °C

5.1: tetrahydrofuran / 1.5 h / 20 °C

6.1: ammonium hydroxide / 0.5 h / 20 °C

With piperidine; ammonium hydroxide; (6,6’-dimethoxy-[1,1 ‘-biphenyl]-2,2’-diyl)bis(bis(3 ,5-dimethyl-phenyl)phosphine); silver(I) acetate; triethylamine; sodium hydroxide; In tetrahydrofuran; 2-methyltetrahydrofuran; methanol; water; ethyl acetate;

DOI:10.1021/op3003213

upstream raw materials:

4-{[(2'S,3'R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-2-oxo-1,2-dihydrospiro[indole-3,3'-pyrrolidine]-5'-carbonyl]amino}-3-methoxybenzoic acid methyl ester

6-chloro-2-oxindole

2-fluoro-3-chlorobenzaldehyde

methyl 3-methoxy-4-aminobenzoate

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