N2-Tritylolmesartan medoxomil
[CAS# 1020157-01-0]

Identification

• Classification: Organic raw materials >> Heterocyclic compound >> Imidazoles
• Name: N2-Tritylolmesartan medoxomil
• Synonyms: (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 5-(2-hydroxypropan-2-yl)-2-propyl-3-[[4-[2-(2-trityltetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylate
• Molecular Formula: C₄₈H₄₄N₆O₆
• Molecular Weight: 800.90
• CAS Registry Number: 1020157-01-0
• SMILES: CCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NN(N=N4)C(C5=CC=CC=C5)(C6=CC=CC=C6)C7=CC=CC=C7)C(=O)OCC8=C(OC(=O)O8)C)C(C)(C)O

Properties

• Density: 1.3±0.1 g/cm³ Calc.^*
• Boiling point: 960.0±75.0 ºC 760 mmHg (Calc.)^*
• Flash point: 534.4±37.1 ºC (Calc.)^*
• Solubility: Insoluble (5.0E^-6 g/L) (25 ºC), Calc.
• Index of refraction: 1.648 (Calc.)^*

^* Calculated using Advanced Chemistry Development (ACD/Labs) Software.

Safety Data

• Hazard Symbols: GHS02;GHS07 Danger
• Hazard Statements: H228-H315-H319
• Precautionary Statements: P240-P210-P241-P264-P280-P302+P352-P370+P378-P337+P313-P305+P351+P338-P362+P364-P332+P313
• Transport Information: UN 1325

Discovory and Applicatios

BN2-Tritylolmesartan medoxomil is a synthetic intermediate used in the multistep chemical preparation of olmesartan medoxomil. It is not intended for direct therapeutic use and does not itself exhibit clinical activity as a pharmaceutical product. Instead, it functions as a protected form of the olmesartan scaffold during manufacture.

The compound incorporates a trityl protecting group at the N2 position, which is employed to control chemoselectivity during key transformations in the synthetic sequence. The use of this protecting group helps prevent undesired side reactions at the tetrazole moiety while allowing other functional groups within the molecule to undergo selective modification. Such protection strategies are common in the synthesis of complex angiotensin receptor blocker intermediates.

N2-Tritylolmesartan medoxomil is typically generated after construction of the biphenyl-tetrazole core and ester functionalities characteristic of the olmesartan framework. Subsequent synthetic steps involve controlled deprotection of the trityl group and further conversion to yield olmesartan medoxomil in its final, pharmacologically active form. These transformations are carried out under carefully optimized conditions to ensure product purity and reproducibility.

In industrial and laboratory settings, the compound is handled solely as a process intermediate. Its role is limited to facilitating efficient synthesis and improving overall yield and selectivity in downstream reactions. It is not formulated, administered, or evaluated as a drug substance, and it is not used outside controlled chemical synthesis workflows.

The identification and use of N2-Tritylolmesartan medoxomil reflect standard practices in modern medicinal chemistry, where temporary structural modification enables precise construction of complex active pharmaceutical ingredients.