intermediate of API

103909-75-7

  • Product Name：Maxacalcitol
  • Molecular Formula：C26H42O4
  • Specifications：99%
  • Molecular Weight：418.617
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Product Details;

CasNo： 103909-75-7

Molecular Formula： C26H42O4

Manufacturer Sells Best Quality Maxacalcitol 103909-75-7 with stock

  • Molecular Formula:C26H42O4
  • Molecular Weight:418.617
  • Vapor Pressure:6.11E-16mmHg at 25°C 
  • Melting Point:122° 
  • Refractive Index:1.549 
  • Boiling Point:581.4 °C at 760mmHg 
  • PKA:14.43±0.40(Predicted) 
  • Flash Point:305.4 °C 
  • PSA：69.92000 
  • Density:1.09 g/cm3 
  • LogP:4.69350 

Maxacalcitol(Cas 103909-75-7) Usage

Brand name

Prezios (Chugai Pharmaceutical Co., Ltd., Japan);Prezios, Oxarol.

InChI:InChI=1/C26H42O4/c1-17-20(15-21(27)16-24(17)28)9-8-19-7-6-12-26(5)22(10-11-23(19)26)18(2)30-14-13-25(3,4)29/h8-9,18,21-24,27-29H,1,6-7,10-16H2,2-5H3/b19-8+,20-9-/t18-,21+,22+,23-,24-,26+/m0/s1

103909-75-7 Relevant articles

Improved and efficient synthesis of Maxacalcitol

Feng, Shi,Cui, Li-Fei,Wei, He-Geng,Zheng, Guo-Jun,Wang, Ya-Ping,Wang, Xiang-Jing,Zhang, Ji,Xiang, Wen-Sheng

, p. 771 - 774 (2014)

Maxacalcitol, the 22-oxa-derivative of 1...

Synthesis of tritiated 1α,25-dihydroxy-22-oxavitamin D3

Watanabe,Akiyama,Kawanishi,Kubodera

, p. 645 - 654 (1995)

Synthesis of two tritiated 1α,25-dihydlo...

Stereoselective synthesis of 22-oxacalcitriol (OCT) and analogues modified at C25

Fall, Yagamare,González, Victoria,Vidal, Beatriz,Mouri?o, Antonio

, p. 427 - 429 (2002)

The stereoselective synthesis of 22-oxac...

A MARTHA calciferol preparation method (by machine translation)

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, (2017/11/04)

The invention belongs to the field of ph...

SYNTHETIC INTERMEDIATE OF MAXACALCITOL, PREPARATION METHOD THEREFOR AND USE THEREOF

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Paragraph 0121; 0122; 0123; 0124, (2016/09/26)

The present invention provides a new met...

Industrial synthesis of maxacalcitol, the antihyperparathyroidism and antipsoriatic vitamin D3 analogue exhibiting low calcemic activity

Shimizu, Hitoshi,Shimizu, Kazuki,Kubodera, Noboru,Mikami, Tetsuhiro,Tsuzaki, Kaname,Suwa, Hiroyuki,Harada, Koji,Hiraide, Akira,Shimizu, Motoki,Koyama, Kaichiro,Ichikawa, Yoshihide,Hirasawa, Daisuke,Kito, Yasushi,Kobayashi, Mio,Kigawa, Masaharu,Kato, Masahiro,Kozono, Toshiro,Tanaka, Hideki,Tanabe, Makoto,Iguchi, Masanori,Yoshida, Mitsutaka

, p. 278 - 287 (2012/12/24)

Maxacalcitol, the 22-oxa-derivative of 1...

103909-75-7 Process route

1α,3β-dihydroxy-androst-5-en-17-one
20998-18-9

1α,3β-dihydroxy-androst-5-en-17-one

maxacalcitol
103909-75-7

maxacalcitol

Conditions
Conditions Yield
Multi-step reaction with 11 steps
1.1: 1H-imidazole / N,N-dimethyl-formamide / 6 h / 20 - 125 °C / Large scale
2.1: potassium tert-butylate / tetrahydrofuran / 4 h / 25 - 30 °C / Large scale
3.1: tetrahydrofuran / 4 h / 20 - 45 °C / Large scale
4.1: sodium hydroxide; dihydrogen peroxide / 1 h / 25 °C / Large scale
5.1: sodium hydride / tetrahydrofuran; mineral oil / 20 °C / Large scale
5.2: 1 h / 20 °C / Reflux; Large scale
6.1: L-Selectride / tetrahydrofuran / 1 h / Reflux; Large scale
7.1: N-Bromosuccinimide; 2,2'-azobis(isobutyronitrile) / n-heptane / 0.25 h / 78 °C
8.1: 2,4,6-trimethyl-pyridine / toluene / 2.5 h / 110 °C / Large scale
9.1: tetrabutyl ammonium fluoride / tetrahydrofuran / 9 h / 66 °C
10.1: tetrahydrofuran / 7 h / 10 °C / Irradiation
11.1: tetrahydrofuran / 85 h / 25 °C
With 1H-imidazole; 2,4,6-trimethyl-pyridine; N-Bromosuccinimide; 2,2'-azobis(isobutyronitrile); potassium tert-butylate; tetrabutyl ammonium fluoride; dihydrogen peroxide; L-Selectride; sodium hydride; sodium hydroxide; In tetrahydrofuran; n-heptane; N,N-dimethyl-formamide; toluene; mineral oil; 2.1: |Wittig Olefination;
Multi-step reaction with 12 steps
1.1: 1H-imidazole / N,N-dimethyl-formamide / 6 h / 20 - 125 °C / Large scale
2.1: potassium tert-butylate / tetrahydrofuran / 4 h / 25 - 30 °C / Large scale
3.1: tetrahydrofuran / 4 h / 20 - 45 °C / Large scale
4.1: sodium hydroxide; dihydrogen peroxide / 1 h / 25 °C / Large scale
5.1: sodium hydride; 15-crown-5 / tetrahydrofuran; mineral oil / 6 h / 0 °C / Large scale
6.1: cerium(III) chloride / tetrahydrofuran / 0.5 h / -15 °C
6.2: 0.5 h / -15 °C
7.1: cerium(III) chloride / tetrahydrofuran / 0.5 h / -15 °C / Large scale
7.2: 0.5 h / -15 °C / Large scale
8.1: N-Bromosuccinimide; 2,2'-azobis(isobutyronitrile) / n-heptane / 0.25 h / 78 °C
9.1: 2,4,6-trimethyl-pyridine / toluene / 2.5 h / 110 °C / Large scale
10.1: tetrabutyl ammonium fluoride / tetrahydrofuran / 9 h / 66 °C
11.1: tetrahydrofuran / 7 h / 10 °C / Irradiation
12.1: tetrahydrofuran / 85 h / 25 °C
With 1H-imidazole; 2,4,6-trimethyl-pyridine; N-Bromosuccinimide; cerium(III) chloride; 15-crown-5; 2,2'-azobis(isobutyronitrile); potassium tert-butylate; tetrabutyl ammonium fluoride; dihydrogen peroxide; sodium hydride; sodium hydroxide; In tetrahydrofuran; n-heptane; N,N-dimethyl-formamide; toluene; mineral oil; 2.1: |Wittig Olefination;
1α,3β-dihydroxy-androst-5-en-17-one
20998-18-9

1α,3β-dihydroxy-androst-5-en-17-one

1α,25-dihydroxy-22-oxavitamin D<sub>3</sub>
103909-75-7,132071-85-3,142864-57-1

1α,25-dihydroxy-22-oxavitamin D3

Conditions
Conditions Yield
Multi-step reaction with 7 steps
1: 94 percent / imidazole, 1-hydroxybenzotriazole / dimethylformamide / 72 h / 50 - 60 °C
2: 1.) NBS; 2.) γ-collidine / 1.) hexane, reflux, 1 h; 2.) xylene, reflux, 1 h
3: 64 percent / dimethylsulfoxide; tetrahydrofuran / Ambient temperature
4: 1.) 9-BBN; 2.) NaOH, H2O2 / 1.) THF, r.t., 16 h
5: 1.) NaH; 2.) O2, PdCl2, CuCl / 1.) xylene, reflux, 18 h; 2.) DMF-H2O, r.t. 19 h
6: 79 percent / tetrahydrofuran / 1 h / 0 °C
With 1H-imidazole; 2,4,6-trimethyl-pyridine; sodium hydroxide; N-Bromosuccinimide; 9-borabicyclo[3.3.1]nonane dimer; dihydrogen peroxide; oxygen; sodium hydride; benzotriazol-1-ol; copper(l) chloride; palladium dichloride; In tetrahydrofuran; dimethyl sulfoxide; N,N-dimethyl-formamide;

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