Keywords:
Drugs -- Design.
;
Pharmaceutical chemistry.
;
Electronic books.
Type of Medium:
Online Resource
Pages:
1 online resource (294 pages)
Edition:
1st ed.
ISBN:
9780470134962
Series Statement:
Wiley Series on Drug Synthesis Series
URL:
https://ebookcentral.proquest.com/lib/geomar/detail.action?docID=304940
Language:
English
Note:
Intro -- THE ART OF DRUG SYNTHESIS -- CONTENTS -- Foreword -- Preface -- Contributors -- 1 THE ROLE OF MEDICINAL CHEMISTRY IN DRUG DISCOVERY -- 1.1 Introduction -- 1.2 Hurdles in the Drug Discovery Process -- 1.3 The Tools of Medicinal Chemistry -- 1.3.1 In Silico Modeling -- 1.3.2 Structure-Based Drug Design (SBDD) -- 1.4 The Role of Synthetic Chemistry in Drug Discovery -- References -- 2 PROCESS RESEARCH: HOW MUCH? HOW SOON? -- 2.1 Introduction -- 2.2 Considerations for Successful Scale-up to Tox Batches and Phase I Material -- 2.3 Considerations for Phase 2 Material and Beyond -- 2.3.1 Reagent Selection -- 2.3.2 Solvent Selection -- 2.3.3 Unit Operations -- 2.3.4 Developing Simple, Effective, Efficient Work-ups and Isolations -- 2.3.5 The Importance of Physical States -- 2.3.6 Route Design and Process Optimization to Minimize COG -- 2.4 Summary -- References -- I CANCER AND INFECTIOUS DISEASES -- 3 AROMATASE INHIBITORS FOR BREAST CANCER: EXEMESTANE (AROMASIN®), ANASTROZOLE (ARIMIDEX®), AND LETROZOLE (FEMARA®) -- 3.1 Introduction -- 3.2 Synthesis of Exemestane -- 3.3 Synthesis of Anastrozole -- 3.4 Synthesis of Letrozole -- References -- 4 QUINOLONE ANTIBIOTICS: LEVOFLOXACIN (LEVAQUIN®), MOXIFLOXACIN (AVELOX®), GEMIFLOXACIN (FACTIVE®), AND GARENOXACIN (T-3811) -- 4.1 Introduction -- 4.1.1 Mechanism of Action -- 4.1.2 Modes of Resistance -- 4.1.3 Structure-Activity Relationship (SAR) and Structure-Toxicity Relationship (STR) -- 4.1.4 Pharmacokinetics -- 4.1.5 Synthetic Approaches -- 4.2 Levofloxacin -- 4.3 Moxifloxacin -- 4.4 Gemifloxacin -- 4.5 Garenoxacin (T-3811): A Promising Clinical Candidate -- References -- 5 TRIAZOLE ANTIFUNGALS: ITRACONAZOLE (SPORANOX®), FLUCONAZOLE (DIFLUCAN®), VORICONAZOLE (VFEND®), AND FOSFLUCONAZOLE (PRODIF®) -- 5.1 Introduction -- 5.2 Synthesis of Itraconazole -- 5.3 Synthesis of Fluconazole.
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5.4 Synthesis of Voriconazole -- 5.5 Synthesis of Fosfluconazole -- References -- 6 NON-NUCLEOSIDE HIV REVERSE TRANSCRIPTASE INHIBITORS -- 6.1 Introduction -- 6.2 Synthesis of Nevirapine -- 6.3 Synthesis of Efavirenz -- 6.4 Synthesis of Delavirdine Mesylate -- References -- 7 NEURAMINIDASE INHIBITORS FOR INFLUENZA: OSELTAMIVIR PHOSPHATE (TAMIFLU®) AND ZANAMIVIR (RELENZA®) -- 7.1 Introduction -- 7.1.1 Relenza -- 7.1.2 Tamiflu -- 7.2 Synthesis of Oseltamivir Phosphate (Tamiflu®) -- 7.3 Synthesis of Zanamivir (Relenza®) -- References -- II CARDIOVASCULAR AND METABOLIC DISEASES -- 8 PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR (PPAR) AGONISTS FOR TYPE 2 DIABETES -- 8.1 Introduction -- 8.1.1 Insulin -- 8.1.2 Sulfonylurea Drugs -- 8.1.3 Meglitinides -- 8.1.4 Biguanides -- 8.1.5 Alpha-Glucosidase Inhibitors -- 8.1.6 Thiazolidinediones -- 8.2 Synthesis of Rosiglitazone -- 8.3 Synthesis of Pioglitazone -- 8.4 Synthesis of Muraglitazar -- References -- 9 ANGIOTENSIN AT(1) ANTAGONISTS FOR HYPERTENSION -- 9.1 Introduction -- 9.2 Losartan Potassium -- 9.2.1 Introduction to Losartan Potassium -- 9.2.2 Synthesis of Losartan Potassium -- 9.3 Valsartan -- 9.3.1 Introduction to Valsartan -- 9.3.2 Synthesis of Valsartan -- 9.4 Irbesartan -- 9.4.1 Introduction to Irbesartan -- 9.4.2 Synthesis of Irbesartan -- 9.5 Candesartan Cilexetil -- 9.5.1 Introduction to Candesartan Cilexetil -- 9.5.2 Synthesis of Candesartan Cilexetil -- 9.6 Olmesartan Medoxomil -- 9.6.1 Introduction to Olmesartan Medoxomil -- 9.6.2 Synthesis of Olmesartan Medoxomil -- 9.7 Eprosartan Mesylate -- 9.7.1 Introduction to Eprosartan Mesylate -- 9.7.2 Synthesis of Eprosartan Mesylate -- 9.8 Telmisartan -- 9.8.1 Introduction to Telmisartan -- 9.8.2 Synthesis of Telmisartan -- References -- 10 LEADING ACE INHIBITORS FOR HYPERTENSION -- 10.1 Introduction -- 10.2 Synthesis of Enalapril Maleate.
,
10.3 Synthesis of Lisinopril -- 10.4 Synthesis of Quinapril -- 10.5 Synthesis of Benazepril -- 10.6 Synthesis of Ramipril -- 10.7 Synthesis of Fosinopril Sodium -- References -- 11 DIHYDROPYRIDINE CALCIUM CHANNEL BLOCKERS FOR HYPERTENSION -- 11.1 Introduction -- 11.2 Synthesis of Nifedipine (Adalat®) -- 11.3 Synthesis of Felodepine (Plendil®) -- 11.4 Synthesis of Amlodipine Besylate (Norvasc®) -- 11.5 Synthesis of Azelnidipine (Calblock®) -- References -- 12 SECOND-GENERATION HMG-CoA REDUCTASE INHIBITORS -- 12.1 Introduction -- 12.2 Synthesis of Fluvastatin (Lescol®) -- 12.3 Synthesis of Rosuvastatin (Crestor®) -- 12.4 Synthesis of Pitavastatin (Livalo®) -- References -- 13 CHOLESTEROL ABSORPTION INHIBITORS: EZETIMIBE (ZETIA®) -- 13.1 Introduction -- 13.2 Discovery Path to Ezetimibe -- 13.3 Synthesis of Ezetimibe (Zetia®) -- References -- III CENTRAL NERVOUS SYSTEM DISEASES -- 14 DUAL SELECTIVE SEROTONIN AND NOREPINEPHRINE REUPTAKE INHIBITORS (SSNRIs) FOR DEPRESSION -- 14.1 Introduction -- 14.2 Synthesis of Venlafaxine -- 14.3 Synthesis of Milnacipran -- 14.4 Synthesis of Duloxetine -- References -- 15 GABA(A) RECEPTOR AGONISTS FOR INSOMNIA: ZOLPIDEM (AMBIEN®), ZALEPLON (SONATA®), ESZOPICLONE (ESTORRA®, LUNESTA®), AND INDIPLON -- 15.1 Introduction -- 15.2 Synthesis of Zolpidem -- 15.3 Synthesis of Zaleplon -- 15.4 Synthesis of Eszopiclone -- 15.5 Synthesis of Indiplon -- References -- 16 α(2)δ LIGANDS: NEURONTIN® (GABAPENTIN) AND LYRICA® (PREGABALIN) -- 16.1 Introduction -- 16.2 Synthesis of Gabapentin -- 16.3 Synthesis of Pregabalin -- References -- 17 APPROVED TREATMENTS FOR ATTENTION DEFICIT HYPERACTIVITY DISORDER: AMPHETAMINE (ADDERALL®), METHYLPHENIDATE (RITALIN®), AND ATOMOXETINE (STRATERRA®) -- 17.1 Introduction -- 17.1.1 Stimulant versus Nonstimulants -- 17.2 Synthesis of Amphetamine.
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17.2.1 Pharmacokinetic Properties of d- and l-Amphetamine -- 17.2.2 Chiral Synthesis of Amphetamine -- 17.3 Synthesis of Methylphenidate -- 17.3.1 Methylphenidate Formulations -- 17.3.2 Chiral Synthesis of Methylphenidate -- 17.4 Synthesis of Atomoxetine -- References -- Index.
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