cas 864750-70-9, 1-(2-(3-((4-carbamoylpiperidin-1-yl)methyl)-N-methylbenzamido)ethyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate

Articles about 864750-70-9Total 8 be found

Preparation method of revefenacin
The invention discloses a preparation method of revefenacin. The preparation method comprises the following steps: (1) carrying out a reductive amination reaction on methyl p-formylbenzoate as shown in a formula I and a compound as shown in a formula II to obtain a compound as shown in a formula III; (2) carrying out a hydrolysis reaction on the compound as shown in the formula III and a sodium hydroxide solution to obtain a compound as shown in a formula IV; (3) carrying out a condensation reaction on the compound as shown in the formula IV, a compound as shown in a formula V, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 1-hydroxybenzotriazole to obtain a compound as shown in a formula VI; (4) carrying out an acid hydrolysis reaction on the compound as shown in the formula VI and a hydrochloric acid solution to obtain a compound as shown in a formula VII; and (5) carrying out a reductive amination reaction on the methyl p-formylbenzoate as shown in the formula VII and a compound as shown in a formula VIII to obtain revefenacin as shown in a formula IX. According to the method provided by the invention, a synthesis route is shortened, a Pd/C hydrogenation high-pressure protecting group removal process is avoided, and the method has the advantages of milder and safer reaction conditions and the like.
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(2021/07/17)

Preparation methods of revefenacin intermediate and revefenacin
The invention relates to a synthesis method of a revefenacin intermediate, which specifically comprises the following steps: in a solvent, enabling piperidin-4-yl [1,1-biphenyl]-2-carbamate to react with methyl(2-oxyethyl) tert-butyl carbamate in the pres
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(2021/05/26)

New rafenacin intermediate, active electrophilic building block thereof and new preparation method of rafenacin
The invention provides a new rafenacin intermediate, an active electrophilic building block thereof and a new preparation method of rafenacin. The new rafenacin intermediate shown as the formula (II) is prepared by sequentially reacting N-methylethanolamine with a compound shown as a formula (III) and a compound shown as a formula (V), and the new rafenacin intermediate shown as the formula (II) is used for activating hydroxyl to prepare an active electrophilic block shown as a formula (VI) and then reacts with a compound shown as a formula (VII) to obtain the rafenacin shown as the formula (I). The synthetic route provided by the invention has the advantages of short reaction steps, low raw material cost, simple reaction operation, mild conditions, high conversion rate, high selectivity and convenient post-treatment, and is more suitable for industrial production.
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(2021/04/26)

Revefenacin intermediate, preparation method thereof and preparation method of revefenacin
The invention relates to the field of pharmaceutical synthesis, in particular to a revefenacin key intermediate (II), and also relates to a preparation method of the intermediate (II) and a method forpreparing revefenacin as shown in a formula (I) through the intermediate (II). The intermediate (II) is prepared from a compound (IV) and a compound (V) which are subjected to an amidation reaction.The revefenacin can be obtained from the intermediate (II) through a substitution reaction. A synthesis route is mild in condition, the conversion rate and selectivity are high, the reaction yield andthe reaction efficiency are high, energy consumption is low, post-treatment is convenient, reaction operation is easy and convenient, and the method for preparing the revefenacin shown in the formula(I) through the intermediate (II) is more suitable for industrial production.
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(2019/12/25)

PROCESS FOR PREPARING A BIPHENYL-2-YLCARBAMIC ACID
The invention provides a process of preparing an intermediate useful in the synthesis of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and a process of preparing a crystalline freebase of the ester.
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(2012/02/01)

CRYSTALLINE FREEBASE FORMS OF A BIPHENYL COMPOUND
The invention provides two crystalline freebase forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester. The invention also provides pharmaceutical compositions comprising the crystallin
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Page/Page column 10-11

(2011/02/18)

CRYSTALLINE FORMS OF A BIPHENYL COMPOUND
The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.
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Page/Page column 33

(2008/06/13)

Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
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Page/Page column 20-21

(2008/06/13)