77083-52-4

Usage

Uses

Used in Pharmaceutical Industry:
(R)-Indapamide is used as an antihypertensive agent for treating high blood pressure. It helps in managing blood pressure by increasing the excretion of sodium and water by the kidneys, leading to a decrease in blood volume and, subsequently, a reduction in blood pressure.
Used in Cardiology:
(R)-Indapamide is used as a diuretic for reducing fluid retention in conditions such as congestive heart failure. By promoting the removal of excess fluid from the body, it alleviates the symptoms and complications associated with congestive heart failure.
Used in Drug Formulation:
(R)-Indapamide is used in the formulation of oral medications, including immediate-release and extended-release tablets, to provide flexible treatment options for patients with high blood pressure and fluid retention issues.

Upstream product

• 1205-30-7 4-chloro-3-sulphamoylbenzoic acid 
• 31529-46-1 1-amino-2,3-dihydro-2-methylindole 
• 70049-77-3 3-(aminosulfonyl)-4-chlorobenzoyl chloride 
• 7440-44-0 pyrographite 
• 63968-75-2 Dehydroindapamide 
• 6872-06-6 2-methyl indoline 
• 26807-65-8 Indapamide 

Downstream Products

• 1108610-87-2 C₈Cl₂N₂O₂*C₁₆H₁₆ClN₃O₃S 

Relevant academic research and scientific papers

Synthesis method of indapamide

The invention discloses a synthesis method of indapamide, which comprises the following synthesis steps: adding 2, 3-dihydro-2-methyl-1H-indole into hydroxylamine-O-sulfonic acid, reacting to obtain 1-amino-2, 3-dihydro--2methyl-1H-indole hydrochloride, dissolving the 1-amino-2, 3-dihydro-2-methyl-1H-indole hydrochloride in an aprotic organic solvent, dropwise adding triethylamine while stirring,adding 4-chloro-3-sulfanilamide benzoic acid and a dehydration condensing agent, and refining by using an isopropanol-aqueous solvent to obtain an indapamide product. According to the synthesis methodof indapamide, an acylating chlorination reaction and a nitroso compound reaction are omitted, the safety coefficient in the synthesis process of indapamide is increased, and generation of harmful substances is reduced; and the effects of short production period and high yield are achieved by changing burdening and reaction paths.

Preparation method of indapamide and midbody thereof

The invention discloses a method for preparing indapamide. The method comprises the following steps: enabling 4-chloro-3-sulfamido-N-(2-methyl-1H-indol-1-base)benzamide to react in an organic solventat 10 to 25 DEG C in the presence of a Brown catalyst, and processing to obtain indapamide. The preparation method is high in conversion rate of the technological process, high in yield, high in purity and capable of meeting the requirement in the pharmaceutical field.

Indapamide synthetic method

The invention relates to a high-quality indapamide preparing method, in particular to a preparing method according to which reaction is easy to control, the cost is low and the yield is high, and belongs to the technical field of bulk pharmaceutical chemical production. By the adoption of the method, the reaction path is changed, 4-chlorine-3-ammonia sulfonyl benzoic acid reacts with t-butyl chloroformate firstly to generate mixed anhydride which then reacts with N-amino-2-methylindoline hydrochloride, thionyl chloride chloroformylation reaction is omitted, safety is improved, environment pollution and equipment corrosion are reduced, cost is reduced, and the yield can be remarkably increased compared with traditional technologies.

DIAZENIUMDIOLATE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.

Compounds of formula (I): wherein: R1 represents a hydrogen atom or a —COOR group, R2 represents a group G or a linear or branched (C1-C6)alkyl group substituted by a group G, wherein G represents a —(CH2)n-A-(CH2)m—B—(CR4R5)p—(CH2)o-R6 group as defined in the description, R3 represents a hydrogen atom, an alkyl group or an NO2 group.

One-pot Synthesis of the Indole Derivative 4-Chloro-3-sulphamoyl-N-(2,3-dihydro-2-methyl-1H-indol-1-yl)benzamide (Indapamide)

New methods for the synthesis the indole derivative, Indapamide (1), using mixed anhydrides of the general formula R1COOCOOR2 (2) or DCC (N,N′-dicyclohexylcarbodiimide) (3), are described.

Application of cyclam-capped β-cyclodextrin-bonded silica particles as a chiral stationary phase in capillary electrochromatography for enantiomeric separations

Two novel types of substituted cyclam-capped β-cyclodextrin (β-CD)-bonded silica particles have been prepared and used as chiral stationary phases in capillary electrochromatography (CEC). The two stationary phases have a chiral selector with three recognition sites: β-CD, cyclam, and the latter's sidearm. They exhibit excellent enantioselectivities in CEC for a wide range of compounds as a result of the cooperative functioning of the anchored β-CD and cyclam. After inclusion of the metal ion (Ni2+) from the running buffer into the substituted cyclams and their sidearm ligands, the bonded stationary phases become positively charged and can provide extra electrostatic interactions with ionizable solutes and enhance the dipolar interactions with some polar neutral solutes. This enhances the host-guest interaction with some solutes and improves chiral recognition and enantioselectivity. These new types of stationary phases exhibit great potential for fast chiral separations in CEC.

Preparation of 4-chloro-3-sulphamoyl-N-(2,3-dihydro-2-methyl-1H-indol-1-yl)-benzamide from 2,3-dihydro-2-methyl-1H-indole and hydroxylamine-O-sulphonic acid

The invention relates to a new process for the industrial preparation of 4-chloro-3-sulphamoyl-N-(2,3-dihydro-2-methyl-1H-indol-1-yl)benzamide from 2,3-dihydro-2-methyl-1H-indole and hydroxylamine-O-sulphonic acid.

Process for the industrial preparation of 4-chloro-3-sulfamoyl-N-(2,3-dihydro-2-methyl-1H-indol-1-yl)benzamide

The invention relates to a new process for the industrial preparation of 4-chloro-3-sulfamoyl-N-(2,3-dihydro-2-methyl-1H-indol-1-yl)benzamide from monochloramine and 2,3-dihydro-2-methyl-1H-indole.

Process for synthesizing certain N-benzoylamino indolines

Compounds of the structure STR1 wherein R is hydrogen, lower alkyl containing 1 to 5 carbon atoms, cycloalkyl containing 3 to 7 carbon atoms, phenyl or phenyl substituted with halogen, trifluoromethyl, or lower alkyl or lower alkoxy having 1 to 4 carbon atoms and R1 is hydrogen, lower alkyl having 1 to 4 carbon atoms, phenyl or phenyl lower alkyl wherein the lower alkyl has 1 to 4 carbon atoms, are formed by cyclizing a compound of the structure STR2 wherein R and R1 are as defined above, in the presence of an acid.