- METHOD FOR PREPARING RIVAROXABAN INTERMEDIATE
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A method for preparing a Rivaroxaban intermediate I is presented, including the following step: in a non-protonic solvent, under the effect of lewis acid, performing cyclization reaction on 4-(4-phenyl isocyanate)morpholine-3-ketone (II) and (S)-epoxy compound (III), the reaction temperature ranging from 20° C. to 60° C., where R is amino replaced by amino protecting group. The preparation method of the present invention has a mild condition, a simple process, a low cost, and high efficiency; the product is easy to purify and the method is applicable to industrial production.
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Paragraph 0036-0038
(2015/02/19)
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- METHOD FOR PREPARING RIVAROXABAN INTERMEDIATE
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Disclosed is a method for preparing a Rivaroxaban intermediate I, comprising the following step: in a non-protonic solvent, under the effect of lewis acid, performing cyclization reaction on 4-(4-phenyl isocyanate)morpholine-3-ketone (II) and (S)-epoxy compound (III), the reaction temperature ranging from 20° C to 60° C, where R is amino replaced by amino protecting group. The preparation method of the present invention has a mild condition, a simple process, a low cost, and high efficiency; the product is easy to purify and the method is applicable to industrial production.
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Paragraph 0024
(2015/03/03)
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- PROCESSES FOR PREPARING RIVAROXABAN
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Processes and intermediates for preparing rivaroxaban, and analogs and derivatives thereof, and pharmaceutically acceptable salts of each of the foregoing, are described herein.
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Page/Page column 15
(2013/10/22)
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- An approach to the anticoagulant agent rivaroxaban via an isocyanate-oxirane cycloaddition promoted by MgI2.etherate
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A convergent and efficient synthesis of anticoagulant rivaroxaban was developed using the cycloaddition of commercially available (R)-epichlorohydrin with 4-(morpholin-3-one)phenyl isocyanate catalysed by MgI2 etherate as the key step, in 22% overall yield.
- Li, Chao,Liu, Yingshuai,Zhang, Yongjun,Zhang, Xingxian
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p. 400 - 401
(2011/10/08)
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- Method for the preparation of rivaroxaban
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The present invention relates to the use of a compound having the formula (II) for the preparation of a compound having the formula (V). Methods of preparing the compound having the formula (V) using the compound having the formula (II) are also described. Individual reaction steps as well as intermediates are additionally claimed.
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Page/Page column 18
(2011/09/12)
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- METHOD FOR THE PREPARATION OF RIVAROXABAN
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The present invention relates to the use of a compound having the formula (II) for the preparation of a compound having the formula (V). Methods of preparing the compound having the formula (V) using the compound having the formula (II) are also described. Individual reaction steps as well as intermediates are additionally claimed.
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Page/Page column 28; 29
(2011/09/15)
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