Antihistamines Pharmaceutical Raw Material Loratadine Powder CAS: 79794-75-5 White Powder

Loratadine CAS: 79794-75-5

Product Name: Loratadine
Synonyms: LORATADINE;LORATADINE-D5;LORATIDINE;CLARATYNE;CLARITIN;ethyl 4-(8-chloro-

5,6-dihydro-11h-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylate;4(8

-CHLORO-5,6-DIHYDRO-11H-BENZO[5,6]CYCLOHEPTA[1,2-B]PYRIDIN-11-YLIDENE)-1-

PIPERIDINECARBOXYLATE;4-(8-CHLORO-5,6-DIHYDRO-11H-BENZO[5,6]CYCLOHEPTA[1,2-B]PYRIDIN-11-

YLIDENE)-1-PIPERIDINECARBOXYLIC ACID ETHYL ESTER
CAS: 79794-75-5
MF: C22H23ClN2O2
MW: 382.88
EINECS: 1308068-626-2
Product Categories: Active Pharmaceutical Ingredients;Intermediates & Fine

Chemicals;Pharmaceuticals;API's;Histamine receptor;Amines;Heterocycles;Pharmaceutical

intermediate;Other APIs

Melting point 134-136°C
RTECS TM6129200
storage temp. 2-8°C
solubility DMSO: 26 mg/mL, soluble
form powder
color white
Water Solubility It is soluble in DMSO (50 mg/ml), ethanol (77 mg/ml at 25°C),

water (<1 mg/ml at 25°C), chloroform, and methanol.
Merck 14,5578
Stability: Stable, but may be heat sensitive - refrigerate. Incompatible with strong

oxidizing agents.

Loratadine Usage And Synthesis
Abstract Loratadine, sold under the brand name Claritin among others.Loratadine

(Claritin) is a long-acting, non-sedating antihistamine that is used for the treatment of

allergies. Histamine is a chemical that causes many of the signs and symptoms of an

allergy. Histamine is released from histamine-storing cells (mast cells) and attaches to

other cells that have receptors for histamine on their surfaces. Histamine stimulates the

cells to release chemicals that produce effects that we associate with allergy, including

welts, itching, and tissue swelling. Loratadine(Claritin) blocks one type of histamine

receptor (the H1 receptor) and thus prevents activation of cells with H1 receptors by

histamine.

Antiallergic Loratadine is a common antiallergic medication, which is a second

generation long-acting tricyclic antihistamine, rapid onset of action is strong, does not

contain hormones, absorbed by the body metabolism with more active desloratadine,

inhibiting histamine H1 receptor by competitively inhibit histamine-induced allergic

symptoms, with no obvious anticholinergic and central inhibition. It is used for the

relief of clinical symptoms of allergic rhinitis related, such as sneezing, runny nose and

nasal itching, eye itching and burning. It is also used to relieve symptoms of chronic

urticaria and other allergic skin diseases.

Drug Interactions Inhibition of hepatic drug-metabolizing enzyme function drugs can

slow the metabolism of the product, such as itraconazole, ketoconazole, Daily with 400 mg

ketoconazole suit, can make the product and its active metabolite to carboxyethyl

loratadine increased plasma concentrations, but it was not observed in the changes of

electrocardiogram (ECG). It can also inhibit the metabolism of loratadine when used with

macrolides, cimetidine, theophylline and other drugs together.

Application

Antihistamines, peripheral nerves are highly selective H1-receptor, the role of strong,

long time. For allergic arthritis, allergic rhinitis.
National second-class anti-allergy drugs, for the relief of seasonal allergic rhinitis

nasal and non-nasal symptoms and relieve chronic urticaria.
Side effects Common side effects include sleepiness, dry mouth, and headache. Serious

side effects are rare and include allergic reactions, seizures, and liver problems. Use

during pregnancy appears to be safe but has not been well studied. It is not recommended in

children less than two years old. It is in the second-generation antihistamine family of

medication.

Preparation Compound (I) (0.05mo1) was dissolved in toluene (450m1), dropwise addition

of ethyl chloroformate (0.15mo1). Canada finished in the sauna heating 2h, and then stirred

at room temperature overnight. Added 800ml water. The benzene layer was separated, washed with water, and dried. Decompression concentrated oil, with petroleum ether after

impregnation with acetonitrile, recrystallization, the yield of loratadine, 64%.

Chemical Properties White Crystalline Solid
Uses antinflammatory, analgesic, antipyretic
Uses Anti-histamine
Uses A nonsedating-type histamine H1-receptor
Biological Activity Peripheral histamine H 1 receptor antagonist (K i = 35 nM); devoid

of central effects. Orally active antiallergic agent.

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