Bromocriptine
B
271
ATC: G02CBO1; N04BCO1
Use: prolactin inhibitor
RN: 25614-03-3 MF: C,,H,,,BrN,O, MW: 654.61 EINECS: 247-128-5
LD,: >800 mglkg (M, p.0.);
72 mglkg (R, i.v.)
CN:
(5'a)-2-bromo-l2'-hydroxy-2'-(l
-methylethyl)-5'-(2-methylpropyl)ergotaman-3',6',18-trione
monomesylate
RN:
22260-51-1 MF: C3,H,oBrN,0,
.
CH,O,S MW: 750.71 EINECS: 244-881
-
1
LD,: 189 mg/kg (M, i.v.); 2502 mglkg (M, p.0.);
10.5 mg/kg (R, i.v.); >2 g/kg (R, p.0.)
Reference(s):
US 3 7.52 814 (Sandoz; 14.8.1973; CH-prior. 31.5.1968).
DAS 1 926 045 (Sandoz; appl. 22.5.1969; CH-prior. 31.5.1968).
ergocryptine
medical use:
US
3
7.52 888 (Sandoz; 14.8.1973; CH-prior. 3 1.5.1968).
Bromocriptine
nasal formulation:
DOS 2 802 113 (Sandoz; appl. 19.1.1978).

Formulation(s):
cps. 5 mg, 10 mg; tabl. 2.5 mg (as mesylate)
Trade Name(sJ:
,
.
D: Kirim (Hormosan) Parlodel (Novartis; 1978)
J:
Parlodel (Novartis; 1979)
Pravidel (Novartis Pharma; GB: Parlodel (Novartis; 1976) USA: Parlodel (Novartis; 1976)
1977) I: Parlodel (Sandoz; 1979)
F:
Bromo-Kin (Irex) Serocryptin (Serono)
Bromopride
ATC: A03FA04
Use: anti-emetic, gastric therapeutic
RN: 4093-35-0 MF: C,,H,,BrN30, MW: 344.25 EINECS: 223-842-2
LD,,: 310 mg/kg (M, p.0.);
545 mg/kg (R, p.0.)
CN:
4-amino-5-bromo-N-[2-(diethylamino)ethyl]-2-methoxybenzamide
272
B
Bromopride
0
methyl 4-ocetamido- N,N-diethyl-
2-rnethoxybenzoate
(I)
ethylenediornine
(11)
Bromopride

L"'
1.
Br,,
CH3COOH
2.
HCI
I11
-b
@
COOH
Br
1
NH2
acetic anhydride
4-amino- methanol methyl 4-amino-
salicylic acid solicylate
dimethyl sulfate
I
Br,.
CH3COOH
2.
HCI
-
Br
k
CH,
K
0
methyl 4-ocetamido-5-
broma-2-methaxybenzoate

yH3
0 0
.
W\I
CH3
K
0
methyl 4-acetamido-
solicylate
(IV)
Brornapride
rn
US 3 177 252 (Soc. &Etudes Scientifiques et Industrielles de 1'Ile-de-France; 6.4. 1965; F-prior. 25.7.1961).
US 3 219 528 (Soc. &Etudes Scientifiques et Industrielles de I'Ile-de-France; 23.1 1.1965; F-prior. 5.8.1960,
4.11 .l96O, 25.7.1961).
US 3 357 978 (Soc. &Etudes Scientifiques et Industrielles de 1'Ile-de-France; 12.12.1967; F-prior. 5.3.1963).
DE 1
233 877 (Soc. dlEtudes Scientifiques et Industrielles de 1'Ile-de-France; appl. 14.7.1962; F-prior.
25.7.1961).
Bromperidol
B
273
alternative synthesis:
DAS 2 102 848 (Delmar; appl. 21.1.1971; USA-prior. 21 .l. 1970).
DAS 2 119 724 (Teikoku Hormone Mfg.; appl. 22.4.197 1
;
J-prior. 24.4.1970).
DAS 2 162 917 (Soc. d'Etudes Scientifiques et Industrielles de l'lle-de-France; appl. 17.12.197 1
;
J-prior.

21.12.1970).
DAS 2 166 118 (Teikoku Hormone Mfg.; appl. 22.4.1971; J-prior. 24.4.1970).
DOS 2 435 222 (Soc. dlEtudes Scientifiques et Industrielles de l'Ile-de-France; appl. 22.7.1974; J-prior.
24.7.1973).
Formulation(s):
amp. 10 mg; cps. 10 mg; drops 13.3 mg
Trade Narne(s):
D: Cascapride (Merck)
I:
Opridan (Locatelli; as Valopride (Synthelabo)
di hydrochloride
monohydrate)
Bromperidol
ATC: N05AD06
Use: antipsychotic, neuroleptic
RN: 10457-90-6 MF: C,,H,,BrFNO, MW: 420.32 EINECS: 233-943-3
LD,,: 18.9 mgkg (M, i.v.); 174 mglkg (M, p.0.);
10 mgkg (R, i.v.); 359 mgkg (R, p.0.)
CN:
4-[4-(4-bromophenyl)-4-hydroxy-l-piperidinyl]-l-(4-fluorophenyl)-l-butanone
monohydrochloride
RN: 59453-24-6 MF: CzIHZ3BrFNO2
.
HCI MW: 456.78
LD,,: 18.9mgkg(R,i.v.); 174mgkg(R, p.0.)
fluorobenzene 4-chlorobutyryl 4-chloro-4'-fluoro-
chloride butyrophenone
(I)
(cf. holoperidol)
4-bromo-a-methyl- form-

styrene aldehyde
pyridine
(11)
1.
HBr
.
HOAc
HO
2. NoOH
D
-
EWWNH
+
I
4-(4-bromapheny1)-
4-hydraxypiperidine
Br&N+
'F
Bromperidol
274
B
Brompheniramine
Reference(s):
US
3
438 991 (Janssen; appl. 15.4.1969; GB-prior. 18.1 1.1959).
DE 1 289 845 (Janssen; appl. 18.4.1959; GB-prior. 22.4.1958).
Niemegeers, C.J.E.; Janssen, P.A.J.: Arzneirn Forsch. (ARZNAD) 24,45 (1974).
Formulation(s):
amp. 5 mglml; drops 2 mglrnl; tabl. 1 mg, 5 mg, 10 mg

Trade Name(s):
D: Impromen (~ansseh; 1983) I: lmpromen (Formenti; J: Impromen (Yoshitomi;
Tesoprel (Organon; 1984) 1989) 1986)
Brompheniramine
ATC:
RO~ABO~
Use: antihistaminic
RN: 86-22-6 MF: C,,H1,BrN,
MW:
319.25 EINECS: 201-657-8
CN:
y-(4-bromophenyl)-N,N-dimethyl-2-pyridinepropanamine
maleate
(1:l)
RN: 980-71-2 MF: C1,H,,BrN,. C4H404 MW: 435.32 EINECS: 213-562-9
LD,,: 3 18 mgkg (R, p.0.)
+
OC'
q
sod~um
amide
4-bromo- 2-chloro- (4-bromopheny1)-
benzyl pyridine (2-pyridyl).
cyanide ocetonitrile
1.
NaNH2
2.
CI-
CH3
Y'

CH3
1.
sodium omide
2. 2-(dimethylomi-
no)ethyl chloride
CN CH,
2-(4-bromopheny1)-4-
dimethylamino-2-(2-
pyridy1)butyronitrile
(I)
Reference(s):
US 2 567 245 (Schering Corp.; 1951; prior. 1948).
US 2 676 964 (Schering Corp.; 1954; prior. 1950).
Formulntion(s):
elixir 4 mg, 2 mgl5 ml; cps. 12 mg
Trade Name(s):
D: Dimegan (Kreussler)
F: Chronotrophir (Sanofi
Winthrop)
DimCgan (Dexo)
Dimetane Expectorant
(Whitehall)
Martigbne (CIBA Vision
0phthalmics)-comb.
Rupton Chronules (Dexo)- USA: Bromfed (Muro; as
comb.
maleate)
GB:
Dimotane (Wyeth)
Dallergy (Laser; as

Dirnotane Plus (Wyeth)- maleate)
comb.
Dimetane (Robins)
I: Ilvin (Bracco; as maleate) Ladrame (ECR; as maleate)
J:
Bromrun (Hokuriku) Poly-Histine (Sanofi; as
maleate)
Broparestrol
B
275
Respahist (Respa; as
maleate)
Rondec (Dura; as maleate)
Ultrabrom (We; as maleate)
Broparestrol
ATC: GO3
Use: estrogen (synthetic)
RN: 479-68-5 MF:
CzzHI,Br MW: 363.30 EINECS: 207-537-1
CN:
1-(2-bromo-l,2-diphenylethenyl)-4-ethylbenzene
I-ethyl-4-phenyl- phenylmognesium 1.2-diphenyl-1-(4- Broporestrol
ocetylbenzene bromide ethylpheny1)ethene
Reference(s):
Dvolaitzky,
M.;
Jacques,
J.:
Bull. Soc. Chim. Biol. (BSCIA3) 40,939 (1958).
Formulation(s):

cream 10
%;
emulsion 5
%
Trade Narne(s1:
F:
Acnestrol (Devimy)-comb.; Longestrol (Laroche I: Acnestrol (Scharper); wfm
wfm Navarron); wfm
Brotizolam
ATC: N05CD09
Use: tranquilizer, hypnotic
RN: 57801-81-7 MF:
C,,H,,BrCIN,S MW: 393.70 EINECS: 260-964-5
LD,: 920 mglkg (M, i.p.1; >10000 mgkg
(M,
p.0.);
1000 mgkg (R, i.p.); >10000 mglkg (R, p.0.)
CN:
2-bromo-4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-[1,2,4]triazolo[4,3-a][1,4]diazepine
1.
"J~~~~~~~
CI
2. H+
0
WZH,),
NCa
+
-
H2N
-1

1.
glycine ethyl
OH
2-chlorobenzoyl- 2.5-dihydroxy-
acetonitrile 1 -3-dithiane
ester
2-omino-3-(2-
chlorobenzoyl)-
thiophene
1. Br2, pyridine
1. bromine
HN
2. phosphorus
5-(2-chl0rophenyl)- pentosulfide 7-brom0-5-(2-
1,3-dihydro-2H-thieno- chloropheny1)- 1.3-
[2,3-el-1.4-diozepin-
2-one
(I)
276
B
Broxvauinoline
1.
N2H4
CH.
H
oJ-
2.
;OXOhcti3
H3C
I1

-
1.
hydrazine
2.
triethyl orthoacetate
I
Brotizolam
Reference(s):
DOS 2 410 030 (Boehringer Ing.; appl. 2.3.1974).
Weber, K.H. et al.: Arzneim Forsch. (ARZNAD)
36,
518 (1986).
alternative synthesis:
DOS 2 503 235 (Boehringer Ing.; appl. 27.1.1975).
DOS 2 533 924 (Boehringer Ing.; appl. 30.7.1975).
synthesis of
5-(2-chloropheny
1)-1,3-dihydro-2H-thieno[2,3-e]-1,4-diazepin-2-one:
DOS
2 221 623 (Hoffmann-La Roche; appl. 3.5.1972; CH-prior. 14.5.1971).
Gewald,
K.:
Chem. Ber. (CHBEAM) 98; 3571 (1965).
Formularion(s):
tabl. 0.25 mg
Trade Name(s):
D: Lendormin (Boehringer I: Lendormin (Boehringer
J:
Lendormin (Nippon
Ing.) Ing.1 Boehringer)

Broxyquinoline
ATC: A07AX01; GOlAC06; POI AAOl
Use: intestinal antiseptic
RN: 521-74-4 MF:
C,H,Br,NO MW: 302.95 EINECS: 208-317-8
LDso: 7420 mgkg (M, p.0.)
CN: 5,6-dibromo-8-quinolinol
oxyquinoline
(q.
v.)
Broxyquinoline
Reference(s):
Bedall, K; Fischer, 0. et al.: Ber. Dtsch. Chem. Ges. (BDCGAS) 14, 1367 (1881).
Zinnei; Fiedler: Arch. Pharm. Ber. Dtsch. Pharm. Ges. (APBDAJ) 291,493 (1958).
DOS 2 515 476 (Chem. Fabrik
Kak; appl. 9.4.1975).
Formulation(s):
ointment 1.5
%
Trade Name(s):
D:
Dysentrocym (Sano1)-
comb.; wfrn
Fenilor Lutschtabletten
(UCB); wfrn
Intestopan (Sandoz)-comb.; F: Colipar (UcCpha); wfrn
wfm Entercine (Robapharm);
Sandoinl-C (Sandoz)- wfm
comb.; wfrn
B

Bucillamine
B
277
Intestopan (Sandoz)-comb.; Norquinol (Norgan)-comb.;
wfm
wfm
Bucillamine
(DE-019; SA-96; Tiobutarit)
RN: 65002-17-7 MF: C7H13N03S2 MW: 223.32
LD50: 2285 mgkg (M, i.p.); 989 mglkg (M, i.v.)
CN:
N-(2-mercapto-2-methyl-1-oxopropyl)-~-cysteine
3.3-dimethyl- benzyl
a-benzylthio-
ocryllc acid
rnercoptan isobutyric acid
(I)
a-benzylthio-
isobutyryl chloride
ATC: MOICC02
Use: immunomodulator. treatment of
Referencefs):
US 4 137 420 (Santen; 30.1.1979; J-prior. 8.3.1976).
DE 2 709 820 (Santen; appl. 7.3.1977; J-prior. 8.3.1976).
medical use as mucolytic:
,
US 4305 958 (Santen; 15.12.1981; J-prior. 8.3.1976).
Formulation(s):
tabl. 100 mg (sugar coated)
Trade

Name(s):
1:
Rimatil (Santen)
rheumatoid arthritis
Bucladesine sodium
ATC: COICE04
Use: cardiotonic, phosphodiesterase
inhibitor, positive inotropic acting
drug
RN: 16980-89-5 MF: Cl,H23N,Na0,P MW: 49 1.37 EINECS: 241-059-4
LD,,: 543 mglkg (M, i.v.); >5 glkg (M, p.0.);
448 mgkg (R, i.v.); >5 gkg
(R,
p.0.)
CN: N-(1-oxybuty1)adenosine cyclic 3',5'-(hydrogen phosphate) 2'-butanoate monosodium salt
278
B
Buclizine
bucladesine
RN: 362-74-3 MF: C,xH,N,OxP MW: 469.39 EINECS: 206-649-8
OH
adenosine cyclic
3',5'-(hydrogen
phosphate)
butyric anhydride
buclodesine
(I)
H
N
o=p-0

0
I
pCH3
0
ONa
I
Budodesine sodium
Reference (s):
JP~
195 096 (Daiichi Seiyaku; appl. 14.2.1975).
JP 51 113 896 (Daiichi Seiyaku; appl. 31.3.1975).
JP
5 239 699 (Daiichi Seiyaku; appl. 26.9.1975).
Formulation(s):
amp. 0.05 mg, 0.2 mg; tabl. 200 mg, 400 mg
Trade Name(s):
J:
Actocin (Daiichi)
Buclizine
(Histabutizine)
ATC: R06AEO1
Use: antiallergic, antihistaminic
RN: 82-95-1 MF:
C2,H3,ClN2 MW: 433.04 EINECS: 201-448-1
CN:
1-[(4-chlorophenyl)phenylmethyl]-4-[[4-(l,1-dimethylethyl)phenyl]methyl]piperazine
dihydrochloride
RN: 129-74-8 MF: C2,H3,C1N,. 2HC1 MW: 505.96 EINECS: 204-962-4
LD,,,: 21 00 mgkg (M, p.0.)
1

Buclosamide
B
279
1
4-chiorobenz-
ethyl piperozine- ethyl 4-(4-chlorobenz-
hydryl chloride
N-carboxylate hydry1)piperazine-1 -carboxylote
(I)
H&'
'CH,
'
+
-
4-tert-butyl-
benzyl chloride
Reference(s):
DE 964 048 (H. Morren; appl. 1952; B-prior. 195 1).
Formulation(s):
tabl. 25 mg
Trade Name(s):
D: Migralave (Temm1er)-
F:
Aphilan (Darcy)
GB:
Migraleve (Pfizer
comb. with paracetamol Consumer)-comb.
Buclosamide
ATC: DOlAE12
Usc: fungicide

RN:
575-74-6
MF:
CI,H,,CINO2
MW:
227.69 EINECS: 209-390-9
CN: N-butyl-4-chloro-2-hydroxybenzamide
methyl 4-chloro- butylamine
salicylate
US
2 923 737 (Hoechst; 2.2.1960; D-prior. 26.1.1956).
Formulation(s):
ointment 10 g1100 g; sol. 10 dl00 ml
Buclosarnide
I
Trade Narne(s):
D:
Jadit (Hoechst)-comb.; Jadit-Hydrocortisone
I:
Jadit (Hoechst)-comb.;
wfm (Hoechst)-comb.; wfm wfm
F:
Jadit (Hoechst); wfm
280
B
Bucloxic acid
Bucloxic acid
(Acide bucloxique)
ATC: NO2
Use: anti-inflammatory

RN: 32808-51-8 MF:
Cl6HI,ClO, MW: 294.78 EINECS: 251-231-0
LD,,: 852
mglkg (M, p.0.);
120 mglkg (R, p.0.)
CN: 3-chloro-4-cyclohexyl-y-oxobenzenebutanoic acid
calcium salt
RN: 32808-53-0 MF: C,,H,,CaCl,O,, MW: 627.62 EINECS: 251-232-6
LD,,: 1700 mgkg (M, p.0.);
175 mglkg (R, p.0.)
cyclohexyl-
succinic 4-0x0-4-(4-cyclohexyl-
benzene
anhydride pheny1)butyric acid
Reference(s):
DE 2 021 445 (Clin-Byla; appl. 2.5.1970; F-prior. 12.5.1969).
GB
1 315 542 (Clin-Byla; appl. 7.5.1970; F-prior. 12.5.1969).
Trade
Nnrnefs):
F:
Esfar (Midy); wfm
Bucloxic acid
ATC: C07A
Use: P-adrenoceptor blocker
RN: 58409-59-9 MF:
C1,H2,NO4
MW: 305.37
LD,,:
31

mglkg (M,
i.v.);
680 mgkg (M, p.0.)
CN:
8-[3-[(1,1-dimethylethy1)amino]-2-hydroxypropoxy]-5-methyl-2H-1-benzopyran-2-one
hydrochloride
RN: 30073-40-6 MF: C,,H2,N04
.
HCI MW: 341.84
H C H
C
1. HBr
'0
'0
HOOC~~OO~
+
@OH
H".04b
OH
CH3 '3'3
rnolic acid 2-methoxy- 5-rnethyl-8-
5-methyl- rnethoxycournorin
phenol