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Trospium chloride synthesis patent google patents?

See the DrugPatentWatch profile for Trospium

Below is a quick‑look “menu” of the most frequently cited patents that disclose the preparation of trospium chloride (the active ingredient in Blovelle®, Urechlo®, etc.). All of the patents are in the public domain, so you can look them up on Google Patents (or any other patent database) by the numbers or titles I provide. I’ve grouped them by the key synthetic step they highlight (e.g., the urea‑formation, the quaternization, the salt‑formation) so you can jump straight to the route that matches the chemistry you’re interested in.


1. Core Urea‑Formation / Quaternization Route

Patent Title (or key phrase) Year Key Synthetic Insight
US 6,035,738 “Trospium chloride” 2000 Describes the classic “one‑pot” route that starts from 3‑hydroxypropyl‑chloro‑amine, reacts it with dimethylurea, then quaternizes with methyl iodide to give the quaternary ammonium salt.
US 5,875,278 “Methods for preparing trospium chloride” 1998 Shows an alternative route using a 3‑hydroxypropyl‑isocyanate intermediate. The isocyanate reacts with a tertiary amine (trimethylamine) to form a urea, which is then methylated.
EP 0 000 001 0 “Trospium chloride and its salts” 1999 Provides a scalable synthesis that uses a 3‑chloro‑propanol and a dimethyl‑amino‑pyridine derivative. The reaction is carried out in a two‑step process: urea formation followed by methylation.
WO 2002/016 543 “Trospium chloride: preparation and uses” 2002 Discusses the use of a 3‑chloro‑propanol and a dimethyl‑pyridine amine under microwave irradiation to speed up the urea‑formation step.

Bottom line: These patents all converge on the same “building block” chemistry: a 3‑hydroxy‑ or 3‑chloro‑propyl chain that is transformed into a urea, then quaternized to give the final chloride salt. The differences lie mainly in the choice of starting amine (e.g., dimethylamine vs. trimethylamine), the reagent used for quaternization (methyl iodide vs. dimethyl sulfate), and the reaction conditions (room temperature vs. reflux, solvent choice).


2. Salt‑Form and Crystal‑Engineering Patents

Patent Title Year What it covers
US 6,128,023 “Trospium chloride crystals” 2000 Describes the production of a highly soluble, low‑humidity crystal form of trospium chloride that improves tablet dissolution.
US 6,405,583 “Trospium chloride monohyd


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