Abstract
Ibandronate and Alendronate/Alendronic acid were prepared by the reaction of the corresponding amino acids (N-methyl-Npentylalanine and γ-aminobutyric acid) with 3.2 equivalents of phosphorus trichloride, in the absence of any phosphorous acid, in methanesulfonic acid at 75 °C for 12 h followed by hydrolysis, pH adjustment and purification. The first intermediate of the reaction sequence is the corresponding chloride (>N(CH2)nC(O)Cl) or mixed ester (>N(CH2)nC(O)OS(O)2Me).
Keywords: Ibandronate, Alendronate, Synthesis, Optimization, Intermediate.
Current Organic Synthesis
Title:Rational Synthesis of Ibandronate and Alendronate
Volume: 10 Issue: 4
Author(s): Gyorgy Keglevich, Alajos Grun, Rita Kovacs, Sandor Garadnay and Istvan Greiner
Affiliation:
Keywords: Ibandronate, Alendronate, Synthesis, Optimization, Intermediate.
Abstract: Ibandronate and Alendronate/Alendronic acid were prepared by the reaction of the corresponding amino acids (N-methyl-Npentylalanine and γ-aminobutyric acid) with 3.2 equivalents of phosphorus trichloride, in the absence of any phosphorous acid, in methanesulfonic acid at 75 °C for 12 h followed by hydrolysis, pH adjustment and purification. The first intermediate of the reaction sequence is the corresponding chloride (>N(CH2)nC(O)Cl) or mixed ester (>N(CH2)nC(O)OS(O)2Me).
Export Options
About this article
Cite this article as:
Keglevich Gyorgy, Grun Alajos, Kovacs Rita, Garadnay Sandor and Greiner Istvan, Rational Synthesis of Ibandronate and Alendronate, Current Organic Synthesis 2013; 10 (4) . https://dx.doi.org/10.2174/1570179411310040007
DOI https://dx.doi.org/10.2174/1570179411310040007 |
Print ISSN 1570-1794 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6271 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Genetic and Non-genetic Determinants of Cardiovascular Disease in South Asians
Current Diabetes Reviews Polyunsaturated Fatty Acids in Pregnancy and Metabolic Syndrome: A Review
Current Pharmaceutical Biotechnology Multiligand Endocytosis and Congenital Defects: Roles of Cubilin, Megalin and Amnionless
Current Pharmaceutical Design Telomere Recombination and the ALT Pathway: A Therapeutic Perspective for Cancer
Current Pharmaceutical Design Gut Microbiome: Lactation, Childbirth, Lung Dysbiosis, Animal Modeling, Stem Cell Treatment, and CNS Disorders
CNS & Neurological Disorders - Drug Targets Meet Our Editorial Board Member
Recent Patents on Anti-Cancer Drug Discovery Potential Application of Gene Therapy to X-Linked Agammaglobulinemia
Current Gene Therapy Current Perspectives on Anti-Aging Interventions
Letters in Drug Design & Discovery Obesity in China: What are the Causes?
Current Pharmaceutical Design Contact Allergy to Topical Corticosteroids: Update and Review on Cross- Sensitization
Recent Patents on Inflammation & Allergy Drug Discovery Biologics: An Update and Challenge of Their Pharmacokinetics
Current Drug Metabolism From Gene to Epigene-Based Therapies Targeting the Vascular Endothelium
Current Vascular Pharmacology Encapsulation in Cell Therapy: Methodologies, Materials, and Clinical Applications
Current Pharmaceutical Biotechnology Dynamic Localization of Hepatocellular Transporters: Role in Biliary Excretion and Impairment in Cholestasis
Current Medicinal Chemistry Acyclonucleosides, Modified Seco-Nucleosides, and Salicyl- or Catechol- Derived Acyclic 5-Fluorouracil O,N-Acetals: Antiproliferative Activities, Cellular Differentiation and Apoptosis
Current Medicinal Chemistry Neutrophil-to-lymphocyte Ratio and Platelet-to-lymphocyte Ratio as Biomarkers for Cardiovascular Surgery Procedures: A Literature Review
Reviews on Recent Clinical Trials Alterations of Sex Differentiation in Males: From Candidate Genes to Diagnosis and Treatments
Current Pharmaceutical Design Preclinical Studies of Alkylureas as Anti-HIV-1 Contraceptive
Current Pharmaceutical Design Thrombotic Complications of Neonates and Children with Congenital Nephrotic Syndrome
Current Pediatric Reviews Monoclonal Antibodies and their Target Specificity Against SARS-CoV-2 Infections: Perspectives and Challenges
Recent Patents on Biotechnology