H1: Virazodone (CAS 163521-12-8) API and Core Synthetic Intermediates | Pharmacological Efficacy, Application Scenarios and Complete Supply Plan

Core Summary

vilazodone (CAS 163521-12-8) is the world’s first SPARI dual-mechanism antidepressant drug approved by FDA, specifically for the treatment of adult severe depression with anxiety symptoms. The complete synthesis route of the drug cannot be separated from three key heterocyclic intermediates: 5-cyanoindole (15861-24-2), 5-(piperazin -1-yl) benzofuran -2-carboxamide (183288-46-2), 3-(4-chlorobutyl)-5-cyanoindole (143612-79-7). Our company can provide high-purity, industrial mass-produced verazodone raw materials and supporting intermediates. The production follows ICH Q7 specification. The products meet the quality standards of European Pharmacopoeia EP and United States Pharmacopoeia USP, and are suitable for the needs of pharmaceutical enterprises in the whole stage of research and development, pilot test and commercial mass production.

Article Directory

1. Basic Introduction of Vilazodone CAS 163521-12-8: Mechanism of Action and Clinical Efficacy

2. The core application field of verazodone API.

3. Comparison Table of Complete Product Parameters (Vilazodone API + Three Intermediates)

4. Synthesis process analysis: the core role of the three intermediates in the preparation of verazodone 4.1 5-cyanoindole (15861-24-2): indole mother nucleus starting material 4.2 3-(4-chlorobutyl)-5-cyanoindole (143612-79-7): indole side chain coupling key intermediate 4.3 5-(piperazine -1-yl) benzofuran -2-carboxamide (183-2-2-amide (183-46-2-2-2-2-2-2-2

5. The supply advantages of our company’s virazodone raw materials and intermediates.

6. Frequently Asked Questions FAQ

7. Summary and consultation channels

H2 1. Virazodone CAS 163521-12-8 Basic Introduction: Mechanism of Action and Clinical Efficacy

classification and mechanism of H3 1.1 drugs

vilazodone is a serotonin partial agonist-reuptake inhibitor (SPARI), which is different from traditional SSRI antidepressants and has dual synergistic pharmacological activities:

1. Selective serotonin reuptake inhibition: strong binding force to serotonin transporter, almost no effect on norepinephrine, dopamine transporter, lower side effects;

2. 5-HT1A receptor partial agonist: precise activation of 5-HT1A receptor, simultaneous improvement of depression accompanied by anxiety, irritability, insomnia and other complications.

The dual pathways synergistically regulate central serotonin nerve conduction, stabilize mood, improve sleep and cognition; there is no significant risk of QT interval prolongation, and cardiovascular safety is better than most similar antidepressants.

H3 1.2 clinical efficacy and product core advantages

· Approved indications: adult major depressive disorder, especially for depressed patients with generalized anxiety disorder;

core advantage 1: the incidence of adverse reactions of sexual dysfunction is much lower than that of traditional SSRI antidepressants, and the clinical tolerance is outstanding;

core advantage 2: oral bioavailability is stable, the finished tablet specification is 10mg/20mg/40mg, and the absorption effect is better when taken with meals;

market application: Europe and the United States central nervous drug mainstream raw materials, overseas pharmaceutical companies, CDMO foundry enterprises demand continued to grow.

H2 2. Core Application Fields of Verazodone API

1. Commercial preparation production: FDA listed drug VIIBRYD verazodone hydrochloride tablets core active raw material drug;

2. Research and development of pharmaceutical laboratory: screening of new antidepressant derivatives and study of pharmacological mechanism of 5-HT receptor;

3. CRO/CDMO large-scale customized production: bulk synthesis of velazodone raw materials, stable supply of three supporting intermediates is the core guarantee of mass production;

4. Basic research in universities and research institutes: experimental materials for neuroscience and animal models of emotional disorders.

H2 3. Comparison Table of Complete Product Parameters (Verazodone API + Three Intermediates)

table

H2 4. Synthesis Process Analysis: Core Role of Three Intermediates in Preparation of Verazodone

the complete chemical name of velazodone: 5-(4-(4-(5-cyano -1H-indole -3-yl) butyl) piperazin -1-yl) benzofuran -2-carboxamide. The molecular structure is composed of indole fragment, piperazine connecting bridge and benzofuran pharmacodynamic fragment. The three intermediates bear the key synthesis steps respectively.

H3 4.1 5-cyanoindole (CAS:15861-24-2): Indole parent nucleus starting material

the base building block of the indole heterocyclic structure of verazodone. Synthesis: Fischer indole alkylation reaction with 1-chloro-4-butanol to generate side chain precursor; 5-position cyano group can enhance the binding activity of the final product to 5-HT1A receptor. Supply value: high purity 5-cyanoindole can greatly reduce the generation of impurities in the alkylation step, simplify the subsequent refining process, and improve the overall yield of downstream intermediate 3-(4-chlorobutyl)-5-cyanoindole.

H3 4.2 3-(4-chlorobutyl)-5-cyanoindole (CAS:143612-79-7): Key Intermediate for Indole Side Chain Coupling

the core precursor connecting the indole ring with the piperazine group is also a process bottleneck intermediate in industrial production. Synthesis: The intramolecular chlorobutyl group provides a leaving chlorine atom, and under the catalysis of potassium iodide, it undergoes nucleophilic substitution with the piperazine ring of 5-(piperazin -1-yl) benzofuran -2-carboxamide, and is directly spliced to generate the complete molecular skeleton of velazodone. Supply advantages: our company optimizes the one-step synthesis process of Fischer indole, simplifies the traditional four-step synthesis route, has a single batch yield ≥ 75%, has no chiral by-products, and meets the mass production demand of ton-level CDMO.

H3 4.3 5-(piperazin -1-yl) benzofuran -2-carboxamide (CAS:183288-46-2): benzofuran piperazine pharmacodynamic fragment

core pharmacophore carrying serotonin reuptake inhibitory activity of verazodone. Synthesis: The free nitrogen atom of piperazine is coupled with the chlorobutyl of the indole intermediate to form a piperazine linkage chain in the middle of the molecule; the benzofuran-2-carboxamide structure is the key unit for binding serotonin transporters. Process advantages: the use of copper catalytic C- N coupling process production, unreacted raw material recovery rate of more than 98%, compared with imported raw materials can effectively reduce the production costs of pharmaceutical companies.

Complete synthetic route combing

5-cyanoindole → alkylation reaction → 3-(4-chlorobutyl)-5-cyanoindole +5-(piperazin -1-yl) benzofuran -2-carboxamide → nucleophilic substitution coupling → crude verazodone → recrystallization purification → high purity verazodone bulk drug (163521-12-8)

H2 5. Our company’s advantages in supplying raw materials and intermediates of verazodone

1. Supporting the whole industry chain: covering the starting raw material 5-cyano indole, two advanced intermediates, velazodone final API one-stop procurement, to meet the needs of CRO, CDMO whole process;

2. Compliance quality inspection system: All products pass the complete set of HPLC, gas GC, heavy metals and residual solvents, and can provide COA quality inspection list, impurity map and DMF filing support;

3. Flexible mass production capacity: laboratory test (100g-5kg) and industrial production line (single batch of 50kg-2000kg) operate simultaneously, and supply in large quantities stably for a long time;

4. Customized supporting services: customized synthesis of derivative intermediates, customized impurity reference substances, low-temperature cold chain logistics of thermal heterocyclic products;

5. Global export qualification: follow ICH Q7 production specifications, can provide a full set of export declaration and testing documents in line with Europe, America and Southeast Asia markets.

H2 6. FAQ

q1: What is the main use of velazodone CAS 163521-12-8?

A1: Vilazodone is FDA-approved oral antidepressant raw material for the treatment of adult severe depression with anxiety symptoms; at the same time, it is widely used in the development of new central nervous drugs and preclinical pharmacological animal experiments.

Q2: What are the three necessary intermediates for the synthesis of vilazodone API?

A2:① 5-cyanoindole CAS 15861-24-2 (indole starting material);② 3-(4-chlorobutyl)-5-cyanoindole CAS 143612-79-7 (indole alkyl coupling intermediate);③ 5-(piperazin -1-yl) benzofuran -2-carboxamide CAS 183288-46-2 (benzofuran piperazine pharmacodynamic fragment). The mainstream industrial synthesis route cannot replace these three core blocks with other raw materials.

Q3: What purity standard does the intermediate need to meet for the large-scale production of velazodone by pharmaceutical companies?

A3: Industrial mass production requires HPLC purity of the three intermediates ≥ 99.0, single unknown impurity ≤ 0.1, and total impurity ≤ 0.5, ensuring that the terminal verazodone bulk drug meets USP and EP pharmacopoeia standards.

Q4: Is it possible to provide laboratory test samples of vilazodone intermediates?

A4: Support 1g/5g/10g scientific research sample sending with complete quality inspection report; At the same time, the synthesis of impurity reference substances and similar derivative intermediates can be customized.

Q5: How long is the delivery cycle for purchasing large quantities of vilazodone intermediates?

A5: Laboratory samples: 3-7 working days; Industrial batch orders above 50kg: 15-25 working days, long-term framework cooperation customers stock stock, priority scheduling and delivery.

H2 7. Summary and consultation channels

vilazodone (CAS 163521-12-8) is a high-growth API for the global central nervous antidepressant track, and the quality of the three core heterocyclic intermediates directly determines API yield, purity and overseas declaration compliance. Our company integrates research and development, pilot test and large-scale production, and supplies a full set of raw materials for the global pharmaceutical enterprises, CRO and CDMO.

If you need quality inspection form COA, technical instruction TDS, quotation sheet or sample test of verazodone bulk drug, 5-cyanoindole, 3-(4-chlorobutyl)-5-cyanoindole, 5-(piperazine -1-yl) benzofuran -2-formamide, please contact our pharmaceutical API & intermediate sales team to obtain professional process technical support and customized supply plan.