Combinatorial Chemistry

Combinatorial chemistry is a technique in which a number of compounds are simultaneously synthesized and has received much focus in the development of drugs. Of the array of products produced, which are called "libraries", those with the desired functions and activity, are easily identified and isolated. Solid-phase syntheses are widely used.
In the solid-phase syntheses, the desired compounds are held by covalent bond to the solid-phase. Therefore, the excess reaction reagents can easily be removed by washing. A variety of compounds can be synthesized quickly upon determination of their synthetic routes. Furthermore, they have the advantage of being capable of automatic synthesis. Currently, the reactions which can be utilized in the solid-phase syntheses are limited, however, other potentially utilizable reactions are vigorously being explored.
In the other synthesis of libraries, the liquid-phase reactions are carried out utilizing conventional organic synthetic reactions. Some developments have been reported and future developments are being anticipated.
We have put on the market various kinds of resins which have widely been utilized through the solid-phase synthetic technique and useful diphenylphosphino polystyrene resin for liquid-phase Mitsunobu reaction. Any of these resins are easy to use in meshes, swelling volume and functional content. For the polymer-supported reagent used for liquid-phase synthesis, please refer to "Polymer-Supported Reagents", and for a group of building blocks intended for the preparation of the combinatorial libraries, please refer to "Chemicals by Class".

Resins

Linkers

TNBS & Chloranil Test Kit

Detection of Amines for Primary Amines (for Detection of Free Amine on the Resins)

Detection of Amines for Primary & Secondary Amines (for Detection of Free Amine on the Resins)

Resins

P1719 P1719 C1679 C1679 H0986 H0986
H0987 H0987 B2368 B2368 B2172 B2172
D2765 D2765 D2766 D2766 A1543 A1543
A2047 A2047 C1642 C1642 C1643 C1643
C1744 C1744 C1745 C1745 C1746 C1746
C1747 C1747 C1750 C1750 C1751 C1751
B2370 B2370 B2371 B2371 B2372 B2372
P1379 P1379 P1432 P1432 S0544 S0544
T1889 T1889
P1719 (Polystyrylmethyl)trimethylammonium Cyanoborohydride cross-linked with 10% DVB (30-50mesh) (2.6-3.0mmol/g)
C1679 2-Chlorotrityl Chloride Resin cross-linked with 1% DVB (200-400mesh) (1.0-1.8mmol/g)
H0986 4-(Hydroxymethyl)phenoxymethyl Polystyrene Resin cross-linked with 1% DVB (200-400mesh) (0.5-1.0mmol/g)
H0987 4-(Hydroxymethyl)phenoxymethyl Polystyrene Resin cross-linked with 1% DVB (200-400mesh) (1.0-2.0mmol/g)
B2368 4-Benzyloxytrityl Alcohol Resin cross-linked with 1% DVB (200-400mesh) (1.4-1.6mmol/g)
B2172 4-Bromo Polystyrene Resin cross-linked with 2% DVB (200-400mesh) (2.6-2.8mmol/g)
D2765 4-Diphenylphosphino Polystyrene Resin cross-linked with 2% DVB (200-400mesh) (1.0-2.0mmol/g)
D2766 4-Diphenylphosphinomethyl Polystyrene Resin cross-linked with 2% DVB (200-400mesh) (0.5-1.0mmol/g)
A1543 Aminomethyl Polystyrene Resin cross-linked with 1% DVB (200-400mesh) (0.5-0.7mmol/g)
A2047 Aminomethyl Polystyrene Resin cross-linked with 1% DVB (200-400mesh) (2.4-3.0mmol/g)
C1642 Chloromethyl Polystyrene Resin cross-linked with 1% DVB (200-400mesh) (0.8-1.3mmol/g)
C1643 Chloromethyl Polystyrene Resin cross-linked with 1% DVB (200-400mesh) (1.6-1.8mmol/g)
C1744 Chloromethyl Polystyrene Resin cross-linked with 1% DVB (100-200mesh) (0.8-1.2mmol/g)
C1745 Chloromethyl Polystyrene Resin cross-linked with 2% DVB (200-400mesh) (2.0-2.5mmol/g)
C1746 Chloromethyl Polystyrene Resin cross-linked with 2% DVB (200-400mesh) (0.8-1.2mmol/g)
C1747 Chloromethyl Polystyrene Resin cross-linked with 2% DVB (100-200mesh) (2.0-2.5mmol/g)
C1750 Chloromethyl Polystyrene Resin cross-linked with 1% DVB (100-200mesh) (2.0-2.5mmol/g)
C1751 Chloromethyl Polystyrene Resin cross-linked with 2% DVB (100-200mesh) (0.8-1.2mmol/g)
B2370 N-(4-Benzyloxytrityl)-N'-(2-nitrobenzenesulfonyl)-1,2-diaminoethane Resin cross-linked with 1% DVB (200-400mesh) (0.9-1.1mmol/g)
B2371 N-(4-Benzyloxytrityl)-N'-(2-nitrobenzenesulfonyl)-1,3-diaminopropane Resin cross-linked with 1% DVB (200-400mesh) (0.9-1.1mmol/g)
B2372 N-(4-Benzyloxytrityl)-N'-(2-nitrobenzenesulfonyl)-1,4-diaminobutane Resin cross-linked with 1% DVB (200-400mesh) (0.9-1.1mmol/g)
P1379 Polystyrene Resin cross-linked with 1% DVB (200-400mesh)
P1432 Polystyrene Resin cross-linked with 1% DVB (100-200mesh)
S0544 Sulfonic Acid Polystyrene Resin cross-linked with 15% DVB (70-90mesh) (2.6-3.0mmol/g)
T1889 Trityl Chloride Resin cross-linked with 1% DVB (200-400mesh) (1.0-1.8mmol/g)

Linkers

D2707 D2707 H1049 H1049 B2322 B2322
H0961 H0961 H0769 H0769
D2707 2,4-Dimethoxy-4'-hydroxybenzophenone
H1049 2-[4-(Hydroxymethyl)-2-nitrophenoxy]acetic Acid Methyl Ester
B2322 2-[4-(tert-Butyldimethylsilyloxymethyl)-2-nitrophenoxy]acetic Acid
H0961 4-(Hydroxymethyl)phenoxyacetic Acid
H0769 4-Hydroxymethylbenzoic Acid

TNBS & Chloranil Test Kit

To conduct the solid phase synthesis, as simple methods TNBS and Chloranil Test are used to detect free amino group on the resin after reaction. Using TNBS Test, the primary amino group can be detected, while Chloranil Test can detect the presence of both primary and secondary amino groups. This method is much safe and simple detection method of free amino group compared to Kaiser Test which requires toxic substance, potassium cyanide fall under the Poisonous and Deleterious Substances Control Law in Japan.

Detection of Amines for Primary Amines (for Detection of Free Amine on the Resins)

D2937 D2937 P1447 P1447
D2937 N,N-Diisopropylethylamine (ca. 10% in N,N-Dimethylformamide) [for Detection of Primary Amines]
P1447 Picrylsulfonic Acid (ca. 1% in N,N-Dimethylformamide) [for Detection of Primary Amines]
T2024 TNBS Test Kit 2,4,6-Trinitrobenzenesulfonic Acid (ca. 1% in DMF) 10ml*1 / N,N-Diisopropylethylamine (ca. 10% in DMF) 10ml*1 [for Detection of Primary Amines]

Detection of Amines for Primary & Secondary Amines (for Detection of Free Amine on the Resins)

C1770 C1770
C1770 Chloranil (ca. 2% in N,N-Dimethylformamide) [for Detection of Primary and Secondary Amines]
C1771 Chloranil Test Kit Chloranil (ca. 2% in DMF) 10ml*1 / Acetaldehyde (ca. 2% in DMF) 10ml*1 [for Detection of Primary and Secondary Amines]


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