- Synthesis of paricalcitol: A novel strategy combining chemical and microbial transformations
-
A novel strategy was developed for the preparation of paricalcitol (1α,25-dihydroxy-19-norvitamin D2) via seven-step chemical transformation and one-step microbial transformation. Using vitamin D2 as a starting material, 1α- and 25-hydroxyl groups of paricalcitol were introduced by Pseudonocardia autotrophica CGMCC5098 at the late stage of the synthesis, allowing us to avoid harsh reaction conditions and tedious steps. The overall yield of paricalcitol was 0.75%.
- Luo,Jiang,Song,Fang,Lu
-
-
Read Online
- Preparation method of paracetamol and injection thereof
-
The invention provides a preparation method of paracetamol, which adopts a raw material 1 as an initial raw material to synthesize paracetamol. Meanwhile, the invention provides a paracetamol injection and a preparation method thereof. The paracetamol injection comprises a 0.0003% w/v-0.0006% w/v of paracetamol as an active ingredient; 0.05-0.1% w/v of a non-ionic active agent, 2-3% w/v of polyethylene glycol 1000 vitamin E succinate, 0.1-0.5% w/v of cholate, 3-5% v/v of ethanol, 1-3% v/v of propylene glycol and the balance of water for injection. According to the paracetamol injection prepared by the invention, the addition amount of an organic solvent can be reduced, and the paracetamol injection is safer to use.
- -
-
Paragraph 0018; 0042; 0044-0070
(2020/08/17)
-
- Preparation method of paricalcitol isomer impurity PY5
-
The invention discloses a preparation method of paricalcitol isomer impurity PY5. The preparation method comprises the following steps: taking (1R, 3aR, 7aR)-1-((2R,5R,E)-5,6-dimethyl heptyl-3-alkene-2-yl)-7a-methyl octahydro-4H-indole-4-ketone as a start
- -
-
Paragraph 0041-0047
(2019/10/23)
-
- Purification method for paricalcitol
-
The invention provides a purification method for paricalcitol. The method does not need any seed crystal; a crude paricalcitol product is dissolved in a mixed solvent of acetone and water, and heatingreflux is carried out so as to allow the crude paricalcitol product to be completely dissolved; and cooling crystallization is carried out at room temperature, wherein a ratio of the usage amounts ofparicalcitol to the mixed solvent is 1: 20 to 1: 80 (g/ml).
- -
-
Paragraph 0110-0111; 0116; 0117
(2018/04/01)
-
- Preparation method for paricalcitol
-
The invention discloses a preparation method for paricalcitol. The preparation method comprises the following steps: (1) subjecting a compound 1 to a hydrolysis reaction so as to prepare a compound 2;(2) subjecting the compound 2 to oxidation with Dess-Martin periodinane so as to prepare a compound 3; (3) subjecting the compound 3 to a reaction with a compound 4 so as to prepare a compound 5; and(4) subjecting the compound 5 to hydrolysis so as to prepare a crude paricalcitol product. Accordinccording to the method of the invention, the content of an epimer impurity B in the crude paricalcitol product is reduced from the source by selecting appropriate reaction conditions, and subsequent purification steps for paricalcitol are simplified; and the preparation method has high yield and little impurities, and is more suitable for large-scale industrial production.
- -
-
-
- Synthesis process of paricalcitol
-
The invention discloses a synthesis process of paricalcitol. The synthesis process of the paricalcitol comprises the steps of adopting nandrolone as a raw material, oxidizing, carrying out wittig reaction, carrying out hydroxy protection, brominating, rearranging, carrying out dehydrobromination, carrying out addition, oxidizing, reducing, carrying out hydroxy deprotection, and opening ring to obtain the paricalcitol. The paricalcitol is used for preventing and treating secondary hyperthyroidism.
- -
-
-
- A new metabolite of Paricalcitol: stereoselective synthesis of (22Z)-isomer of 1α,25-dihydroxy-19-norvitamin D2
-
Stereoselective synthesis of (22Z)-isomer of Paricalcitol, an analog of 1,25-dihydroxyergocalciferol, an active form of vitamin D2 (Ergocalciferol) has been described. The two key critical synthetic steps involved are Julia–Lythgoe's Wittig–Hor
- Samala, Ramakrishna,Sharma, Somesh,Basu, Manas K.,Mukkanti,Porstmann, Frank
-
supporting information
p. 1309 - 1312
(2018/03/26)
-
- Synthesis and crystallographic study of 1,25-dihydroxyergocalciferol analogs
-
The hybrid analogs of 1,25-dihydroxyergocalciferol (PRI-5201 and PRI-5202) were synthesized as potential anticancer agents using a convergent strategy. The analogs were designed by combining a 19-nor modification of the A-ring with the homologated and rig
- Pietraszek, Anita,Malińska, Maura,Chodyński, Michal,Krupa, Malgorzata,Krajewski, Krzysztof,Cmoch, Piotr,Wo?niak, Krzysztof,Kutner, Andrzej
-
p. 1003 - 1014
(2013/10/21)
-
- NEW SYNTHONES FOR PREPARATION OF 19-NOR VITAMIN D DERIVATIVES
-
The present invention discloses the synthone of Formula (I), wherein R1 and R2 are the same or different and represent independently hydrogen atom or hydroxyl protecting group, and its use for preparation of 19-nor vitamin D derivatives of general Formula (IV), wherein represents single or double bond, p represents an integer 0 to 3, R1 and R2 represent independently hydrogen atom or hydroxyl protecting group, R3 represents hydrogen atom, CH3 or hydroxyl group, R4, R5 and R6 represent independently hydrogen atom, C1-C3-alkyl or hydroxyl group or two of R4, R5 and R6 substituents altogether form cyclopropyl group, in particular for preparation of paricalcitol.
- -
-
-
- METHODS FOR PRODUCING PARICALCITOL
-
The present invention is directed to novel processes for the preparation of paricalcitol to novel intermediates used in these processes, and to processes for preparation of the novel intermediates.
- -
-
Page/Page column 126
(2010/04/03)
-
- Process for preparation of paricalcitol and intermediates thereof
-
The invention relates to a novel process for the preparation of Paricalcitol and intermediates thereof.
- -
-
Page/Page column 17
(2009/03/07)
-
- Novel synthesis of 1α,25-dihydroxy-19-norvitamin D from 25-hydroxyvitamin D
-
19-Norvitamin D analogs 3a and 3b were synthesized from 25-hydroxyvitamin D, obtained via a bioconversion method. The synthetic route features a highly regio- and stereoselective hydroboration reaction to afford 25-hydroxy-3,5-cyclopropyl-vitamin D deriva
- Toyoda, Asako,Nagai, Hazuki,Yamada, Tomonari,Moriguchi, Yusuke,Abe, Junko,Tsuchida, Toshio,Nagasawa, Kazuo
-
experimental part
p. 10002 - 10008
(2010/02/27)
-
- PROCESS FOR PRODUCTION OF 1-HYDROXY-19-NORCYCLOVITAMIN D DERIVATIVE AND INTERMEDIATE FOR THE PRODUCTION
-
A cyclovitamin D derivative produced from 25-hydroxyvitamin D is reacted with osmium tetraoxide or a permanganic acid salt to produce a 10,19-diolcyclovitamin D derivative. The 10,19-diolcyclovitamin D derivative is reacted with a perhalogenic acid salt o
- -
-
Page/Page column 37
(2009/08/16)
-