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Finerenone is a novel mineralocorticoid receptor antagonist that has the effect of delaying the progression of chronic kidney disease. Some people may be aware of two other mineralocorticoid receptor antagonists: the diuretic antihypertensive drug spironolactone, and eplerenone.Finerenone is their cognate derivative and is a third-generation mineralocorticoid receptor antagonist.

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  • 1050477-31-0 Structure
  • Basic information

    1. Product Name: Finerenone (BAY 94-8862)
    2. Synonyms: Finerenone (BAY 94-8862)
    3. CAS NO:1050477-31-0
    4. Molecular Formula: C21H22N4O3
    5. Molecular Weight: 378.42438
    6. EINECS: N/A
    7. Product Categories: N/A
    8. Mol File: 1050477-31-0.mol
  • Chemical Properties

    1. Melting Point: N/A
    2. Boiling Point: 554.7±50.0 °C(Predicted)
    3. Flash Point: N/A
    4. Appearance: /
    5. Density: 1.29±0.1 g/cm3(Predicted)
    6. Refractive Index: N/A
    7. Storage Temp.: N/A
    8. Solubility: N/A
    9. PKA: 14.76±0.40(Predicted)
    10. CAS DataBase Reference: Finerenone (BAY 94-8862)(CAS DataBase Reference)
    11. NIST Chemistry Reference: Finerenone (BAY 94-8862)(1050477-31-0)
    12. EPA Substance Registry System: Finerenone (BAY 94-8862)(1050477-31-0)
  • Safety Data

    1. Hazard Codes: N/A
    2. Statements: N/A
    3. Safety Statements: N/A
    4. WGK Germany:
    5. RTECS:
    6. HazardClass: N/A
    7. PackingGroup: N/A
    8. Hazardous Substances Data: 1050477-31-0(Hazardous Substances Data)

1050477-31-0 Usage

Uses

Finerenone is the first non-steroidal selective mineralocorticoid receptor antagonist, which can be used for the treatment of diabetic nephropathy, chronic kidney disease and end-stage renal disease. It can reduce the proteinuria of patients and improve the glomerular filtration rate.

Biological activity

Finerenone (FIN, BAY 94-8862) is a highly selective, orally active, nonsteroidal antagonist of mineralocorticoid receptor (MR) with IC50 of 18 nM. Finerenone has the potential to study cardio-renal diseases such as type 2 diabetes and chronic kidney disease.

In vivo

Finerenone (BAY 94-8862) lowers albuminuria by >40% and significantly reduces systolic blood pressure (SBP) in Munich Wistar Fr?mter (MWF) rat.

Check Digit Verification of cas no

The CAS Registry Mumber 1050477-31-0 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,5,0,4,7 and 7 respectively; the second part has 2 digits, 3 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1050477-31:
(9*1)+(8*0)+(7*5)+(6*0)+(5*4)+(4*7)+(3*7)+(2*3)+(1*1)=120
120 % 10 = 0
So 1050477-31-0 is a valid CAS Registry Number.

1050477-31-0SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 15, 2017

Revision Date: Aug 15, 2017

1.Identification

1.1 GHS Product identifier

Product name (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide

1.2 Other means of identification

Product number -
Other names Finerenone

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:1050477-31-0 SDS

1050477-31-0Downstream Products

1050477-31-0Relevant articles and documents

Synthetic method of fenerenone and intermediate thereof

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Paragraph 0037-0039, (2022/04/06)

The invention provides a novel synthetic method of a fenerenone intermediate. The method comprises the following steps: (1) in the presence of an acid and in an inert solvent or solvent-free condition, carrying out a reaction on diethyl malonate, 4-cyano-2-methoxybenzaldehyde and 4-amino-5-methyl-2-hydroxypyridine to prepare a compound 1; (2) carrying out alkylation reaction on the compound 1 obtained in the step (1) and triethyl orthoformate in an inert solvent or solvent-free condition under acid catalysis to obtain a compound 2; (3) reducing the compound 2 obtained in the step (2) through a reducing agent to obtain a compound 3; (4) in the presence of a catalyst, splitting the compound 3 and alcohol by a chemical method to prepare a chiral compound 4; the reaction formula is shown in the specification. By applying the technical scheme provided by the invention, a chiral column splitting method is avoided, so that the cost is reduced; by adopting a chemical method for splitting, the raw material loss is reduced, the post-treatment is simple, and the industrial large-scale production is facilitated.

PROCESS FOR PREPARING (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1,6-NAPHTHYRIDINE-3-CARBOXAMIDE ENABLED BY A CATALYTIC ASYMMETRIC HANTZSCH ESTER REDUCTION

-

, (2022/01/06)

The present invention relates to a novel process for preparing (4S)-4-(4-Cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide by an asymmetric Hantzsch ester reduction of racemic 4-(4-Cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,6-naphthyridine-3-carboxamide.

METHOD FOR THE PREPARATION OF (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1-6-NAPHTHYRIDINE-3-CARBOX-AMIDE BY RACEMATE SEPARATION BY MEANS OF DIASTEREOMERIC TARTARIC ACID ESTERS

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Paragraph 0151; 0162-0169; 0174; 0176-0182; 0191-0247, (2021/06/04)

The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and also to the preparation of the enantiomer (Ia) by racemat

Enantioselective Total Synthesis of (?)-Finerenone Using Asymmetric Transfer Hydrogenation

Aggarwal, Varinder K.,Farrar, Elliot H. E.,Gandhamsetty, Narasimhulu,Grayson, Matthew N.,Lerchen, Andreas,Platzek, Johannes,Winter, Nils

, p. 23107 - 23111 (2020/12/01)

(?)-Finerenone is a nonsteroidal mineralocorticoid receptor antagonist currently in phase III clinical trials for the treatment of chronic kidney disease in type 2 diabetes. It contains an unusual dihydronaphthyridine core. We report a 6-step synthesis of (?)-finerenone, which features an enantioselective partial transfer hydrogenation of a naphthyridine using a chiral phosphoric acid catalyst with a Hantzsch ester. The process is complicated by the fact that the naphthyridine exists as a mixture of two atropisomers that react at different rates and with different selectivities. The intrinsic kinetic resolution was converted into a kinetic dynamic resolution at elevated temperature, which enabled us to obtain (?)-finerenone in both high yield and high enantioselectivity. DFT calculations have revealed the origin of selectivity.

METHOD FOR THE PREPARATION OF (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1-6-NAPHTHYRIDINE-3-CARBOXAMIDE AND RECOVERY OF (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1-6-NAPHTHYRIDINE-3-CARBOXAMIDE BY ELECTROCHEMICAL METHODS

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Paragraph 0300-0313; 0323-0329, (2018/09/16)

The present invention relates to a novel process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and recovering (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) proceeding from (4R)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula ent-(I)

METHOD FOR THE PREPARATION OF (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1-6-NAPHTHYRIDINE-3-CARBOXAMIDE AND THE PURIFICATION THEREOF FOR USE AS AN ACTIVE PHARMACEUTICAL INGREDIENT

-

, (2018/09/16)

The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I)

METHOD FOR THE PREPARATION OF (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1-6-NAPHTHYRIDINE-3-CARBOX-AMIDE AND THE PURIFICATION THEREOF FOR USE AS AN ACTIVE PHARMACEUTICAL INGREDIENT

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Paragraph 0184-0190, (2017/08/26)

The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and also the preparation and use of the crystalline polymorph I of (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I).

SUBSTITUTED 4-ARYL-1,4-DIHYDRO-1,6-NAPHTHYRIDINAMIDES AND USE THEREOF

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Paragraph 0512-0515, (2016/10/17)

1,6-Naphthyridine or 8-azaquinazoline derivatives (I) are new. 1,6-Naphthyridine or 8-azaquinazoline derivatives of formula (I) are new. D : N or CR 4>; R 4> : H, F, CF 3 or 1-4C alkyl; Ar : 5-R 5>-6-R 6>-2-methyl-4-oxo-4H-1-benzopyran-8-yl; 3-R 6>-4-R 8>-1-naphthyl optionally substituted with 1-3 of R 7>; 7-R 6>-8-R 8>-5-quinolinyl optionally substituted with 1-2 of R 7>; or 2-R 9>-3-R 10>-4-R 8>-5-R 6>-phenyl; R 5> : H, F, Cl, CN, NO 2, CF 3 or 1-4C alkyl; R 6> : H or F; R 7> : halo, 1-4C alkyl, CF 3, 1-4C alkoxy or OCF 3; R 8> : CN or NO 2; R 9> : H or halo; optionally fluorinated 1-4C alkyl, 1-4C alkoxy, 1-4C alkylthio of di(1-4C alkyl)amino; or phenyl optionally substituted with halo, 1-4C alkyl or CF 3; R 10> : H, halo or 1-4C alkyl; R 1> : optionally fluorinated 1-4C alkyl; R 2> : 1-6C alkyl optionally substituted with 3-7C cycloalkyl or F; or SO 2R 11>; R 11> : 1-6C alkyl, CF 3 or 3-7C cycloalkyl; or phenyl or heteroaryl optionally substituted with 1-2 of halo, CN, 1-4C alkyl, CF 3, 1-4C alkoxy and/or OCF 3; R 3> : H, F, CF 3 or 1-4C alkyl. An independent claim is also included for a process for preparing (I). [Image] ACTIVITY : Hypotensive; Cardiant; Hepatotropic; Nephrotropic; Cerebroprotective. MECHANISM OF ACTION : Mineralocorticoid receptor (MR) antagonist. 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2-methyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide had an IC 50 of 35 nM when tested on cells expressing a GAL4-MR chimera.

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